General Information of Drug Therapeutic Target (DTT) (ID: TTKWM86)

DTT Name Opioid receptor mu (MOP)
Synonyms hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
Gene Name OPRM1
DTT Type
Successful target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
OPRM_HUMAN
TTD ID
T47768
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Function
Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B. Also couples to adenylate cyclase stimulatory G alpha proteins. The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4. Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization. Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction. The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins. The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation. Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling. Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling. Endogenous ligands induce rapid desensitization, endocytosis and recycling whereas morphine induces only low desensitization and endocytosis. Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties. Involved in neurogenesis. Isoform 12 couples to GNAS and is proposed to be involved in excitatory effects. Isoform 16 and isoform 17 do not bind agonists but may act through oligomerization with binding-competent OPRM1 isoforms and reduce their ligand binding activity. Receptor for endogenous opioids such as beta-endorphin and endomorphin.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Estrogen signaling pathway (hsa04915 )
Morphine addiction (hsa05032 )
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Peptide ligand-binding receptors (R-HSA-375276 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
23 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alfentanil DMVO0UB Anaesthesia 9A78.6 Approved [2]
Alvimopan DMHR8KW Gastrointestinal disease DE2Z Approved [3]
Anileridine DMBAUED Pain MG30-MG3Z Approved [4]
Anileridine Hydrochloride DMC128O Pain MG30-MG3Z Approved [5]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [6]
Diphenoxylate DMO5SZX Diarrhea ME05.1 Approved [7]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [8]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [9]
Hydrocodone DMQ2JO5 Allergic rhinitis CA08.0 Approved [10]
Hydromorphone DMHP21E Back pain ME84.Z Approved [11]
Levomethadyl Acetate DM06HG5 Opioid dependence 6C43.2Z Approved [12]
Levopropoxyphene Napsylate Anhydrous DMECB4H Cough MD12 Approved [5]
Methadyl Acetate DMIRMVB Opioid dependence 6C43.2Z Approved [13]
Methylnaltrexone bromide DMZTGN2 Opioid-induced constipation DB32.1 Approved [14]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [15]
Naldemedine Tosylate DMGD3YH Opioid-induced constipation DB32.1 Approved [16]
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [17]
Naloxegol DML0B41 Opioid-induced constipation DB32.1 Approved [18]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [19]
Oxycodone DMXLKHV Osteoarthritis FA00-FA05 Approved [20]
Propoxyphene Hydrochloride DMMSOLA Pain MG30-MG3Z Approved [21]
Remifentanil DMZTXCH Anaesthesia 9A78.6 Approved [1]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [14]
------------------------------------------------------------------------------------
⏷ Show the Full List of 23 Approved Drug(s)
16 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GRT-6005 DMHN3PG Diabetic neuropathy 8C0Z Phase 3 [22]
Morphine-6-glucuronide DMPVW6H Pain MG30-MG3Z Phase 3 [23]
NKTR-181 DM45DS8 Chronic low back pain MG30.02 Phase 3 [24]
ALKS33 DMF3QN1 Alcohol dependence 6C40.2 Phase 2 [25]
Carfentanil DM7ADGX N. A. N. A. Phase 2 [26]
Met-enkephalin DMSZFTP Pain MG30-MG3Z Phase 2 [27]
OPNT001 DMYG1ZQ Eating disorder 6B82 Phase 2 [28]
ORP-101 DMSH20P Irritable bowel syndrome DD91.0 Phase 2 [29]
TD-1211 DMTJMK5 Opioid-induced constipation DB32.1 Phase 2 [30]
AIKO-150 DMW9ZFS Opioid dependence 6C43.2Z Phase 1 [11]
Cyt-1010 DMTV09A Pain MG30-MG3Z Phase 1 [31]
GSK1521498 DM2L7TH Obesity 5B81 Phase 1 [32]
MCP-201 DMW9YOJ Pain MG30-MG3Z Phase 1 [33]
NOCICEPTIN DMUPA7C Headache 8A80-8A84 Phase 1 [34]
SALVINORIN A DMJ3HQY Cerebral vasospasm BA85.Z Phase 1 [35]
TRV734 DMHD8CF Chronic pain MG30 Phase 1 [36]
------------------------------------------------------------------------------------
⏷ Show the Full List of 16 Clinical Trial Drug(s)
19 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ADL-5945 DMQM54P Constipation DD91.1 Discontinued in Phase 2 [37]
BCH-2687 DM6ANFC Pain MG30-MG3Z Discontinued in Phase 2 [38]
DPI-3290 DMKGXT2 Pain MG30-MG3Z Discontinued in Phase 2 [39]
Dynorphin a DMT2WVP N. A. N. A. Discontinued in Phase 2 [40]
Frakefamide DMTRBU4 Pain MG30-MG3Z Discontinued in Phase 2 [41]
MIRFENTANIL HYDROCHLORIDE DMT6IUR Pain MG30-MG3Z Discontinued in Phase 2 [42]
Transdur-sufentanil DMX32RC Pain MG30-MG3Z Discontinued in Phase 2 [43]
TREFENTANIL HYDROCHLORIDE DME85Z9 Pain MG30-MG3Z Discontinued in Phase 2 [44]
ADL-7445 DML1AUZ Constipation DD91.1 Discontinued in Phase 1 [37]
KN-203 DM37IH5 Urinary incontinence MF50.2 Discontinued in Phase 1 [45]
VP004 DMXK8FQ Substance use disorder 6C4Z Discontinued in Phase 1 [46]
443C81 DMQ4X7Y Asthma CA23 Terminated [49]
BCH-150 DMNH9A6 Gastrointestinal disease DE2Z Terminated [50]
BIPHALIN DMKNS10 N. A. N. A. Terminated [51]
DBO-11 DM8GHT2 Cancer related pain MG30 Terminated [23]
DBO-17 DMFJ3UW Cancer related pain MG30 Terminated [23]
Sameridine DMEN6YO Pain MG30-MG3Z Terminated [52]
SB-213698 DM58PKG N. A. N. A. Terminated [53]
SNF-9007 DM4CNM9 N. A. N. A. Terminated [54]
------------------------------------------------------------------------------------
⏷ Show the Full List of 19 Discontinued Drug(s)
2 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GNTI DMTJRLU Obesity 5B81 Preclinical [47]
LY-25582 DM2N637 Obesity 5B81 Preclinical [48]
------------------------------------------------------------------------------------
449 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+/-)-nantenine DM0L3GE Discovery agent N.A. Investigative [55]
(+/-)-TRANS-U-50488 METHANESULFONATE DMM2QOX Discovery agent N.A. Investigative [56]
(-)-cyclorphan DMC8WS4 Discovery agent N.A. Investigative [57]
(-)-eseroline DMJD34Q Discovery agent N.A. Investigative [56]
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) DMSCQ64 Discovery agent N.A. Investigative [58]
1,10-bis-(Dmt-Tic-amino)decane DM9UGFQ Discovery agent N.A. Investigative [59]
1,4-bis-(Dmt-Tic-amino)butane DMLBHXN Discovery agent N.A. Investigative [59]
1,6-bis-(Dmt-Tic-amino)hexane DMRG2CU Discovery agent N.A. Investigative [59]
1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane DMMUZK9 Discovery agent N.A. Investigative [59]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol DMOR9EK Discovery agent N.A. Investigative [60]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol DMV3FSH Discovery agent N.A. Investigative [60]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol DMLYO8P Discovery agent N.A. Investigative [60]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol DMTANPG Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol DMWHMNY Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol DMXZFPB Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol DM1QYS8 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol DMIT7SH Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol DM0BQYX Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol DMWYG8K Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol DME0BJD Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol DMRNZD6 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol DMXT894 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol DMJDUM5 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol DMMB2GV Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol DMJ8F60 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol DMNOZR2 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-benzylpiperidin-4-ol DMVBR36 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-butylpiperidin-4-ol DMRN7SC Discovery agent N.A. Investigative [61]
1-benzhydryl-4-cyclohexylpiperidin-4-ol DMZVSYD Discovery agent N.A. Investigative [61]
1-benzhydryl-4-cyclopropylpiperidin-4-ol DMM94Y2 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-ethoxy-4-phenylpiperidine DM6PIL2 Discovery agent N.A. Investigative [60]
1-benzhydryl-4-hexylpiperidin-4-ol DMUK95S Discovery agent N.A. Investigative [61]
1-benzhydryl-4-isopropylpiperidin-4-ol DMGYCQ3 Discovery agent N.A. Investigative [61]
1-benzhydryl-4-m-tolylpiperidin-4-ol DMVJH1S Discovery agent N.A. Investigative [61]
1-benzhydryl-4-methoxy-4-phenylpiperidine DMBG0N8 Discovery agent N.A. Investigative [60]
1-benzhydryl-4-o-tolylpiperidin-4-ol DMVUMSF Discovery agent N.A. Investigative [61]
1-benzhydryl-4-p-tolylpiperidin-4-ol DM679RC Discovery agent N.A. Investigative [61]
1-benzhydryl-4-phenyl-4-propoxypiperidine DMEB968 Discovery agent N.A. Investigative [60]
1-benzhydryl-4-phenylpiperidin-4-ol DM7KU1X Discovery agent N.A. Investigative [62]
1-benzhydryl-4-tert-butylpiperidin-4-ol DMM5DTF Discovery agent N.A. Investigative [61]
1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol DMLRS8I Discovery agent N.A. Investigative [63]
1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol DMB1NF0 Discovery agent N.A. Investigative [63]
14-O-phenylpropylnaltrexone DMI7LXH Discovery agent N.A. Investigative [64]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine DMUQWPZ Discovery agent N.A. Investigative [65]
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine DM174HN Discovery agent N.A. Investigative [65]
17-methyl-4'-methyldihydromorphinone DMMEB64 Discovery agent N.A. Investigative [66]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate DMI4WCQ Discovery agent N.A. Investigative [65]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide DMW75IF Discovery agent N.A. Investigative [67]
2-Benzylaminomethyl-3-hydroxymorphinan DM6EMGJ Discovery agent N.A. Investigative [65]
2-Hydroxymethyl-3-hydroxymorphinan DM4LMPD Discovery agent N.A. Investigative [65]
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone DMWTP7Y Discovery agent N.A. Investigative [59]
3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone DM2Y4A6 Discovery agent N.A. Investigative [59]
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone DMJR983 Discovery agent N.A. Investigative [59]
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone DMEQBS3 Discovery agent N.A. Investigative [59]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole DM2YKHI Discovery agent N.A. Investigative [68]
3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol DM1DQGJ Discovery agent N.A. Investigative [69]
3-desoxy-3-carboxamidonaltrexone DMBNA0V Discovery agent N.A. Investigative [25]
3-Methylfentanyl DMX71N9 Discovery agent N.A. Investigative [70]
3-Methylthiofentanyl DMC153X Discovery agent N.A. Investigative [71]
4-(4-((phenethylamino)methyl)phenoxy)benzamide DM0QRJ3 Discovery agent N.A. Investigative [72]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [73]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide DM0XDG6 Discovery agent N.A. Investigative [74]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol DM8ZRAE Discovery agent N.A. Investigative [75]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol DMVCIJB Discovery agent N.A. Investigative [60]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol DM6EFLV Discovery agent N.A. Investigative [60]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol DMISTXQ Discovery agent N.A. Investigative [60]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol DM1GRWY Discovery agent N.A. Investigative [60]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol DMZQ7DP Discovery agent N.A. Investigative [60]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol DMALIQ8 Discovery agent N.A. Investigative [60]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol DMFV0JC Discovery agent N.A. Investigative [60]
4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol DM2MPWC Discovery agent N.A. Investigative [60]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol DM5R6T4 Discovery agent N.A. Investigative [60]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide DMZYE8W Discovery agent N.A. Investigative [72]
6-(2-benzylisoindolin-5-yloxy)nicotinamide DMUD2R9 Discovery agent N.A. Investigative [48]
6-(2-phenethylisoindolin-5-yloxy)nicotinamide DMQOJBN Discovery agent N.A. Investigative [48]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide DMEM1BA Discovery agent N.A. Investigative [72]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide DM9VD4W Discovery agent N.A. Investigative [48]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide DMDKOWP Discovery agent N.A. Investigative [48]
6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide DMOSDM2 Discovery agent N.A. Investigative [72]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide DMDTMB7 Discovery agent N.A. Investigative [72]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol DMYMJHF Discovery agent N.A. Investigative [76]
6-desoxonaltrexone DMGZQNS Discovery agent N.A. Investigative [25]
6beta-naltrexol HCl DMZ8PBE Discovery agent N.A. Investigative [77]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide DMQMSZR Discovery agent N.A. Investigative [78]
8-carboxamidocyclazocine DMD18V5 Discovery agent N.A. Investigative [79]
Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 DMVDH4I Discovery agent N.A. Investigative [80]
Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 DMKVU8P Discovery agent N.A. Investigative [80]
Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG DM512OP Discovery agent N.A. Investigative [81]
Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG DMAHQIV Discovery agent N.A. Investigative [81]
Ac-RYYRIK-K-(NH2)-YAFGYPS DM2ND3U Discovery agent N.A. Investigative [81]
Ac-RYYRIK-K-(NH2)-YRFB DMNA3F4 Discovery agent N.A. Investigative [81]
Ac-YGGFL-NH2 DMC0TU5 Discovery agent N.A. Investigative [82]
ADC-5510 DMV761D Movement disorder 8A07-8A0Z Investigative [20]
AIKO-151 DMUQ6XH Opioid dependence 6C43.2Z Investigative [20]
AIKO-152 DML5Y1Q Opioid dependence 6C43.2Z Investigative [20]
AKUAMMINE DM8DYWN Discovery agent N.A. Investigative [56]
AMINOFENTANYL DM7Y6AL Discovery agent N.A. Investigative [83]
Antanal 1 DMGDZ6Q Discovery agent N.A. Investigative [84]
Antanal 2 DMZSUHY Discovery agent N.A. Investigative [84]
Benzyl derivative of M6G DMX8W4G Discovery agent N.A. Investigative [85]
Beta-endorphin DM7XC6B Discovery agent N.A. Investigative [86]
Beta-funaltrexamine DMJORFK Discovery agent N.A. Investigative [87]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate DM0WKNI Discovery agent N.A. Investigative [57]
BREMAZOCINE DM3EIBU Discovery agent N.A. Investigative [88]
BUTORPHAN DM82KPQ Discovery agent N.A. Investigative [89]
C6S DM4LIHQ Discovery agent N.A. Investigative [90]
CARBOXYFENTANYL DMI7Q61 Discovery agent N.A. Investigative [91]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH DMQUB19 Discovery agent N.A. Investigative [92]
Clocinnamox DMZLMJH Discovery agent N.A. Investigative [64]
CODEINONE DM08WPL Discovery agent N.A. Investigative [93]
CTAP DMLON9K Discovery agent N.A. Investigative [94]
CTOP DM7VAJX Discovery agent N.A. Investigative [95]
CYCLAZOCINE DMC6DAZ Discovery agent N.A. Investigative [89]
CYCLORPHAN DMB1U8V Discovery agent N.A. Investigative [89]
CYPRODIME DMJXCVA Discovery agent N.A. Investigative [96]
C[L-Ala-D-pro-L-Phe-D-trp] DMHXTWK Discovery agent N.A. Investigative [80]
C[L-mTyr-D-pro-L-Phe-D-trp] DMNHSR0 Discovery agent N.A. Investigative [80]
C[L-Phe-D-pro-L-mTyr-D-trp] DM82ZOM Discovery agent N.A. Investigative [80]
C[L-Phe-D-pro-L-Phe-D-trp] DM0NTU5 Discovery agent N.A. Investigative [80]
C[L-Phe-D-pro-L-Phe-L-trp] DMCY4L0 Discovery agent N.A. Investigative [80]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] DM4M3OP Discovery agent N.A. Investigative [80]
C[L-Phe-D-pro-L-Tyr-D-trp] DMADSBT Discovery agent N.A. Investigative [80]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] DMLB6UA Discovery agent N.A. Investigative [80]
C[L-Tyr-D-pro-L-Phe-D-trp] DM7OIY8 Discovery agent N.A. Investigative [80]
D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 DMUJC97 Discovery agent N.A. Investigative [97]
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) DM2EFLA Discovery agent N.A. Investigative [97]
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) DMPQHRC Discovery agent N.A. Investigative [97]
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 DMMXA5K Discovery agent N.A. Investigative [97]
DADLE DMRM0OW Discovery agent N.A. Investigative [98]
DAMGO DMS1DVA Discovery agent N.A. Investigative [99]
DC6S DMX9FOB Discovery agent N.A. Investigative [90]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 DMU287Q Discovery agent N.A. Investigative [100]
DELTORPHIN DMHOT9P Discovery agent N.A. Investigative [101]
DELTORPHIN-II DM9ZWRK Discovery agent N.A. Investigative [102]
Deprotected cogener of M6G DMH340E Discovery agent N.A. Investigative [85]
DERMORPHIN DMCYQHO Discovery agent N.A. Investigative [81]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 DMSN87T Discovery agent N.A. Investigative [100]
DIHYDROAKUAMMINE DMW1ALX Discovery agent N.A. Investigative [56]
Dihydromorphine DM4TR0D Discovery agent N.A. Investigative [103]
Dimepheptanol DMRMHE8 Discovery agent N.A. Investigative [76]
Dimethylthiambutene DM7EKAF Discovery agent N.A. Investigative [104]
Diprenorphine DMIXPU6 Discovery agent N.A. Investigative [105]
DM3A6S DM7YXKL Discovery agent N.A. Investigative [90]
DM3B6S DML68UF Discovery agent N.A. Investigative [90]
DM6S DMAJ0Q8 Discovery agent N.A. Investigative [90]
Dmt-Pro-3,5Dmp-Phe-NH2 DM5WEFK Discovery agent N.A. Investigative [106]
Dmt-Pro-Dmp-Phe-NH2 DMGUIR1 Discovery agent N.A. Investigative [106]
Dmt-Pro-Dmt-Phe-NH2 DM4VEU2 Discovery agent N.A. Investigative [106]
Dmt-Pro-Emp-Phe-NH2 DM06VGY Discovery agent N.A. Investigative [106]
Dmt-Pro-Imp-Phe-NH2 DMXUI1J Discovery agent N.A. Investigative [106]
Dmt-Pro-Mmp-Phe-NH2 DM78PFN Discovery agent N.A. Investigative [106]
Dmt-Pro-Phe-D-1-Nal-NH2 DM0VCWA Discovery agent N.A. Investigative [107]
Dmt-Pro-Phe-D-2-Nal-NH2 DMRJVE8 Discovery agent N.A. Investigative [107]
Dmt-Pro-Phe-Phe-NH2 DMM8BIE Discovery agent N.A. Investigative [106]
Dmt-Pro-Tmp-Phe-NH2 DMEMQAK Discovery agent N.A. Investigative [106]
Dmt-Pro-Trp-D-2-Nal-NH2 DMKEV5U Discovery agent N.A. Investigative [107]
Dmt-Sar-Phe-D-2-Nal-NH DMHRT0F Discovery agent N.A. Investigative [108]
DPDPE DMIRSNA Discovery agent N.A. Investigative [99]
DSLET DMSTOB0 Discovery agent N.A. Investigative [20]
dynorphin B DMSPVLM Discovery agent N.A. Investigative [20]
Dynorphin(1-8) DMM92LG Discovery agent N.A. Investigative [109]
ELAEOCARPENINE DMRHSCQ Discovery agent N.A. Investigative [110]
ENDOMORPHIN 2 DMOQWBU Discovery agent N.A. Investigative [111]
ENDOMORPHIN-1 DMBJUEM Discovery agent N.A. Investigative [112]
Endomorphins DMI2RQS Inflammation 1A00-CA43.1 Investigative [20]
ethylketocyclazocine DM9YRCU Discovery agent N.A. Investigative [20]
Ethylmorphine DM0YROF Discovery agent N.A. Investigative [113]
ETONITAZENE DMFR1SE Discovery agent N.A. Investigative [114]
Etorphine DM79YZN Discovery agent N.A. Investigative [115]
FALCARINDIOL DMLOV18 Discovery agent N.A. Investigative [116]
FLUPERAMIDE DMEGL84 Discovery agent N.A. Investigative [117]
H-2',6'-dimethyltyrosine-Tic-OH DMYOADQ N. A. N. A. Investigative [118]
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH DM7IEU2 Discovery agent N.A. Investigative [118]
H-Aba-ala-Gly-Phe-leu-OH DM61G0I Discovery agent N.A. Investigative [27]
H-Aba-ala-Gly-Phe-Met-OH DMKD94Q Discovery agent N.A. Investigative [27]
H-Aba-Gly-Gly-Phe-Leu-OH DMH1L3P Discovery agent N.A. Investigative [27]
H-Aba-ser-Gly-Phe-Leu-Thr-OH DMFE3J4 Discovery agent N.A. Investigative [27]
H-Apa-ala-Gly-Phe-leu-OH DM5SUYP Discovery agent N.A. Investigative [27]
H-Cdp-ala-Gly-Phe-leu-OH DMV751G Discovery agent N.A. Investigative [27]
H-Cdp-Gly-Gly-Phe-Leu-OH DMVEB8C Discovery agent N.A. Investigative [27]
H-Cdp-ser-Gly-Phe-Leu-Thr-OH DMCDLTV Discovery agent N.A. Investigative [27]
H-Cpa-Gly-Gly-Phe-Met-NH2 DMU6PV8 Discovery agent N.A. Investigative [27]
H-Cpa-Gly-Gly-Phe-Met-OH DM154G2 Discovery agent N.A. Investigative [27]
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 DMY4QE6 Discovery agent N.A. Investigative [119]
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 DM8GC36 Discovery agent N.A. Investigative [119]
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 DMNAE6J Discovery agent N.A. Investigative [119]
H-Dmt-Aba-Gly-NH-CH2-Bid DM9WJZK Discovery agent N.A. Investigative [120]
H-Dmt-Aba-Gly-NH-CH2-Ph DM61CMS Discovery agent N.A. Investigative [120]
H-Dmt-Aba-Gly-NH-Ph DMCQYIJ Discovery agent N.A. Investigative [120]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 DMHK70B Discovery agent N.A. Investigative [121]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH DMM9EPQ Discovery agent N.A. Investigative [121]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 DM1ZDJ6 Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH DMC3APN Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 DMY97TN Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH DMGPAM0 Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 DMOI1U5 Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH DMZBFJ5 Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 DMNS1GX Discovery agent N.A. Investigative [122]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH DMM9TUR Discovery agent N.A. Investigative [122]
H-Dmt-Tic-Asp-N(Me)-Ph DM4JP8L Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Asp-NH-Bzl DMBKOJG Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Asp-NH-Ph DM3W9FQ Discovery agent N.A. Investigative [123]
H-Dmt-Tic-D-Asp-N(Me)-Ph DM483BG Discovery agent N.A. Investigative [123]
H-Dmt-Tic-D-Asp-NH-Ph DMUG7X1 Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) DMQSRPD Discovery agent N.A. Investigative [58]
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 DMF52SH Discovery agent N.A. Investigative [124]
H-Dmt-Tic-Glu-NH2 DM8A573 Discovery agent N.A. Investigative [124]
H-Dmt-Tic-Gly-N(Me)-Ph DMHYKBC Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Gly-NH-Bzl DMM39YW Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Gly-NH-CH2-Bid DMH6JOU Discovery agent N.A. Investigative [120]
H-Dmt-Tic-Gly-NH-Ph DMIZ28H Discovery agent N.A. Investigative [123]
H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph DM2TY43 Discovery agent N.A. Investigative [125]
H-Dmt-Tic-Lys(Ac)-NH-Ph DMZH9P5 Discovery agent N.A. Investigative [125]
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph DMP8HFA Discovery agent N.A. Investigative [125]
H-Dmt-Tic-Lys(Z)-NH-Ph DMBXGLA Discovery agent N.A. Investigative [125]
H-Dmt-Tic-Lys-NH-CH2-Ph DMDJ9PE Discovery agent N.A. Investigative [125]
H-Dmt-Tic-Lys-NH-Ph DMT3Y6E Discovery agent N.A. Investigative [125]
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H DMMJ9YN Discovery agent N.A. Investigative [126]
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H DM0BGNE Discovery agent N.A. Investigative [126]
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H DMQ586T Discovery agent N.A. Investigative [126]
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid DMAU2H6 Discovery agent N.A. Investigative [125]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid DM5TZ1J Discovery agent N.A. Investigative [123]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) DMIDLPT Discovery agent N.A. Investigative [123]
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) DMNEAQ9 Discovery agent N.A. Investigative [123]
H-Dmt-Tic-NH-CH2-Boa DM4IUCW Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH2-Bta DMZ8C0U Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH2-CH2-NH2 DMYJAW4 Discovery agent N.A. Investigative [128]
H-Dmt-Tic-NH-CH2-Imid DMJ2F8M Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH2-ImidPh DMKGIQJ Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH2-Indl DMNY3A1 Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH2-Indn DMZWUFK Discovery agent N.A. Investigative [127]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid DM8PJ92 Discovery agent N.A. Investigative [125]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid DMQ4ILK Discovery agent N.A. Investigative [125]
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid DMQEDP5 Discovery agent N.A. Investigative [125]
H-mCpa-ala-Gly-Phe-leu-OH DM17QMV Discovery agent N.A. Investigative [27]
H-mCpa-ser-Gly-Phe-Leu-Thr-OH DM8OUHV Discovery agent N.A. Investigative [27]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH DMA2CZL Discovery agent N.A. Investigative [92]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 DM48XV0 Discovery agent N.A. Investigative [129]
H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 DMXPJHB Discovery agent N.A. Investigative [129]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 DM7QAES Discovery agent N.A. Investigative [129]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 DMZSTL5 Discovery agent N.A. Investigative [129]
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 DMI7CR9 Discovery agent N.A. Investigative [130]
H-Tyr-c[D-Orn-Aic-Glu]-NH2 DMOTI0P Discovery agent N.A. Investigative [130]
H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 DMN2AQO Discovery agent N.A. Investigative [131]
H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 DM6ZHWS Discovery agent N.A. Investigative [131]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 DMDF9AS Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac DM4VBDW Discovery agent N.A. Investigative [133]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H DM0J8P6 Discovery agent N.A. Investigative [134]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo DMW50ZQ Discovery agent N.A. Investigative [134]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H DMF82C1 Discovery agent N.A. Investigative [134]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc DM6UWKL Discovery agent N.A. Investigative [133]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H DMSXD63 Discovery agent N.A. Investigative [133]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac DMRUD37 Discovery agent N.A. Investigative [133]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc DMIPXCZ Discovery agent N.A. Investigative [133]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H DMFSKDM Discovery agent N.A. Investigative [134]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 DM2K16M Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl DMRE4ZI Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 DM1ESMZ Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl DM56KDV Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl DMH3YKR Discovery agent N.A. Investigative [132]
H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 DMSX8CH Discovery agent N.A. Investigative [131]
H-Tyr-Gly-Gly-Phe-Met-NH2 DM6D0ZS Discovery agent N.A. Investigative [27]
H-Tyr-Pro-Ala-Phe-NH2 DMP0CRD Discovery agent N.A. Investigative [82]
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 DMQUNGC Discovery agent N.A. Investigative [58]
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 DM326GJ Discovery agent N.A. Investigative [58]
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H DMXQUKJ Discovery agent N.A. Investigative [128]
H-Tyr-Tic-Cha-Phe-OH DM1VFLG Discovery agent N.A. Investigative [122]
H-Tyr-Tic-Phe-Phe-OH DMI0U87 Discovery agent N.A. Investigative [122]
HERKINORIN DMJXBWV Discovery agent N.A. Investigative [35]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 DM25KZE Discovery agent N.A. Investigative [135]
ICI-199441 DMEWZ80 Discovery agent N.A. Investigative [136]
KETOCYCLAZOCINE DM0RC8M Discovery agent N.A. Investigative [137]
KIN-3031 DMHEOBY Pain MG30-MG3Z Investigative [20]
KIN-4044 DMO8JQM Non-small-cell lung cancer 2C25.Y Investigative [20]
KNT-5 DMZF3E9 Discovery agent N.A. Investigative [138]
KNT-62 DM9M5HC Discovery agent N.A. Investigative [17]
KNT-63 DM0U5N9 Discovery agent N.A. Investigative [17]
KRP-100 DMJX9E1 Discovery agent N.A. Investigative [20]
KRP-110 DME9HZC Constipation DD91.1 Investigative [20]
Leucine-enkephalin DMT2CZK Discovery agent N.A. Investigative [109]
LOFENTANIL DMR2WQE Discovery agent N.A. Investigative [139]
M3A6S DMJK1RE Discovery agent N.A. Investigative [90]
M3B6S DMAHGBF Discovery agent N.A. Investigative [90]
M3IBu6S DM0UOF1 Discovery agent N.A. Investigative [90]
M3P6S DMXT87E Discovery agent N.A. Investigative [90]
M3Pr6S DMMC8RN Discovery agent N.A. Investigative [90]
M3S DMWADOY Discovery agent N.A. Investigative [90]
M6G thiosaccharide analogue DMRB4YV Discovery agent N.A. Investigative [85]
M6S DMFCUN4 Discovery agent N.A. Investigative [90]
MC-CAM DMAHN4L Discovery agent N.A. Investigative [140]
MCL-117 DMQIGZ7 Discovery agent N.A. Investigative [57]
MCL-139 DMQ1BDZ Discovery agent N.A. Investigative [57]
MCL-144 DMW7ZF8 Discovery agent N.A. Investigative [141]
MCL-145 DMJXU67 Discovery agent N.A. Investigative [57]
MCL-147 DMH5SMT Discovery agent N.A. Investigative [142]
MCL-149 DMTWY94 Discovery agent N.A. Investigative [142]
MCL-153 DMCPW5F Discovery agent N.A. Investigative [143]
MCL-154 DM3PIHV Discovery agent N.A. Investigative [143]
MCL-182 DM39YW1 Discovery agent N.A. Investigative [142]
MCL-183 DMVR51Z Discovery agent N.A. Investigative [142]
MCL-428 DMXBHE4 Discovery agent N.A. Investigative [144]
MCL-429 DM1XH04 Discovery agent N.A. Investigative [144]
MCL-431 DMISHCW Discovery agent N.A. Investigative [144]
MCL-432 DMPOFAR Discovery agent N.A. Investigative [144]
MCL-433 DMD3OAQ Discovery agent N.A. Investigative [144]
MCL-434 DMR31VO Discovery agent N.A. Investigative [144]
MCL-435 DMLSYD9 Discovery agent N.A. Investigative [144]
MCL-443 DM8LTQ4 Discovery agent N.A. Investigative [144]
MCL-444 DM8HALS Discovery agent N.A. Investigative [144]
MCL-445 DMR2K4F Discovery agent N.A. Investigative [142]
MCL-446 DMXF73G Discovery agent N.A. Investigative [142]
MCL-447 DMSTGNH Discovery agent N.A. Investigative [142]
MCL-448 DMSJGA9 Discovery agent N.A. Investigative [142]
MCL-449 DMQ890N Discovery agent N.A. Investigative [144]
MCL-450 DM7I6U8 Discovery agent N.A. Investigative [145]
MCL-451 DMP523A Discovery agent N.A. Investigative [145]
MCL-457 DMORMGU Discovery agent N.A. Investigative [142]
MCL-458 DMZN93Y Discovery agent N.A. Investigative [142]
METAZOCINE DMB6T23 Discovery agent N.A. Investigative [146]
MM3A6S DMB74MS Discovery agent N.A. Investigative [90]
MM3B6S DM9PGQI Discovery agent N.A. Investigative [90]
MORPHICEPTIN DM9A1RY Discovery agent N.A. Investigative [111]
MORPHINONE DM9LQIA Discovery agent N.A. Investigative [93]
MR-1029 DMS7FC6 Discovery agent N.A. Investigative [147]
MR-1526 DM5WMXJ Discovery agent N.A. Investigative [147]
MR-2034 DMF04AG Discovery agent N.A. Investigative [137]
MR-2266 DMXWSIU Discovery agent N.A. Investigative [147]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea DMFRQ2U Discovery agent N.A. Investigative [65]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea DMHANU5 Discovery agent N.A. Investigative [65]
N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 DMFNCQ1 Discovery agent N.A. Investigative [148]
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 DM8QTSU Discovery agent N.A. Investigative [148]
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 DMSC9FV Discovery agent N.A. Investigative [148]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine DM7SEM1 Discovery agent N.A. Investigative [65]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine DMLP9VM Discovery agent N.A. Investigative [65]
N-isobutylnoroxymorphone DMN1FIU Discovery agent N.A. Investigative [149]
NalBzOH DM0CP36 Discovery agent N.A. Investigative [90]
naloxonazine DM8ZMNH Discovery agent N.A. Investigative [95]
Naltrexone-6-alpha-ol DMRAN5O Discovery agent N.A. Investigative [137]
naltriben DMNDOLZ Discovery agent N.A. Investigative [20]
NCT-400 DM09UFT Major depressive disorder 6A70.3 Investigative [20]
NE-2 DMILP0F Pain MG30-MG3Z Investigative [20]
NORBINALTORPHIMINE DMLYZOG Discovery agent N.A. Investigative [150]
normorphine DMYQGFJ Discovery agent N.A. Investigative [20]
NRP290 DMC9XJA Pain MG30-MG3Z Investigative [20]
NRT-300 DM3IWP5 Pain MG30-MG3Z Investigative [20]
O-DESMETHYL TRAMADOL DM8ZG2I Discovery agent N.A. Investigative [137]
ORIPAVINE DMPQGUL Discovery agent N.A. Investigative [93]
OXYMORPHINDOLE DMTP4S2 Discovery agent N.A. Investigative [114]
Oxymorphone semicarbazone hydrochloride DMTSM61 Discovery agent N.A. Investigative [109]
PHENAZOCINE DMCTVMI Discovery agent N.A. Investigative [137]
PL017 DMICVXN Discovery agent N.A. Investigative [94]
PTI-601 DMQUSXK Pain MG30-MG3Z Investigative [20]
quadazocine DM2Q6JY Discovery agent N.A. Investigative [20]
RTI-5989-31 DMZO1QC Discovery agent N.A. Investigative [151]
SB-0304 DMOZX0D Discovery agent N.A. Investigative [152]
Semorphone DM1C5GZ Discovery agent N.A. Investigative [153]
SL-3111 DM0UE28 Discovery agent N.A. Investigative [154]
SN-11 DMA0JZM Discovery agent N.A. Investigative [53]
SN-23 DM6O0PD Discovery agent N.A. Investigative [53]
SN-28 DMB8TJC Discovery agent N.A. Investigative [155]
SOMATOSTATIN DMIOFQE Acromegaly 5A60.0 Investigative [97]
SPIROINDANYLOXYMORPHONE DMNJVZU Discovery agent N.A. Investigative [156]
THEBAINE DMRCD3O Discovery agent N.A. Investigative [93]
TQ-1017 DMEF32D Pain MG30-MG3Z Investigative [157]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH DMBU4KJ Discovery agent N.A. Investigative [92]
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 DMIWPKB Discovery agent N.A. Investigative [158]
Tyr-(R)-Aba-Gly-Phe-NH2 DMDQJUO Discovery agent N.A. Investigative [159]
Tyr-(R)-spiro-Aba-Gly-Phe-NH2 DMHNM3K Discovery agent N.A. Investigative [159]
Tyr-(S)-Aba-Gly-Phe-NH2 DMYZ792 Discovery agent N.A. Investigative [159]
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 DMT316S Discovery agent N.A. Investigative [159]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 DM0D1Z5 Discovery agent N.A. Investigative [54]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DMPH1G0 Discovery agent N.A. Investigative [54]
Tyr-D-Ala-Gly-NMePhe DM2XRZL Discovery agent N.A. Investigative [87]
Tyr-D-Ala-Gly-Phe-Met-NH2 DMC7LND Discovery agent N.A. Investigative [51]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl DMWOP9N Discovery agent N.A. Investigative [160]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc DMB2TCF Discovery agent N.A. Investigative [133]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 DMUXMVQ Discovery agent N.A. Investigative [54]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 DMREJ69 Discovery agent N.A. Investigative [54]
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 DMTPLNZ Discovery agent N.A. Investigative [161]
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 DMC4NO5 Discovery agent N.A. Investigative [162]
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 DM4FASR Discovery agent N.A. Investigative [161]
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 DMB9A46 Discovery agent N.A. Investigative [161]
Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 DMLC0NW Discovery agent N.A. Investigative [161]
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 DM4YTFP Discovery agent N.A. Investigative [162]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 DMY9NIJ Discovery agent N.A. Investigative [54]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DMQREP2 Discovery agent N.A. Investigative [54]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 DMZ24LN Discovery agent N.A. Investigative [54]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 DMPSJ72 Discovery agent N.A. Investigative [54]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 DMIWMN6 Discovery agent N.A. Investigative [54]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DM2CEWT Discovery agent N.A. Investigative [54]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 DMKM81A Discovery agent N.A. Investigative [54]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 DMZOTGM Discovery agent N.A. Investigative [54]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 DMM9H07 Discovery agent N.A. Investigative [54]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 DMN7290 Discovery agent N.A. Investigative [54]
Tyr-Pro-3,5Dmp-Phe-NH2 DMDCJWU Discovery agent N.A. Investigative [106]
Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 DMH08O3 Discovery agent N.A. Investigative [158]
Tyr-Pro-D-Phe-D-Pro-NH2 DM4ZJR5 Discovery agent N.A. Investigative [158]
Tyr-Pro-D-Phe-Pro-NH2 DMCTSNE Discovery agent N.A. Investigative [158]
Tyr-Pro-D-Phg-Phe-NH2 DMEDVRN Discovery agent N.A. Investigative [163]
Tyr-Pro-Dmp-Phe-NH2 DMNXCHT Discovery agent N.A. Investigative [106]
Tyr-Pro-Dmt-Phe-NH2 DMOU43H Discovery agent N.A. Investigative [106]
Tyr-Pro-Emp-Phe-NH2 DMUKE43 Discovery agent N.A. Investigative [106]
Tyr-Pro-Hfe-Phe-NH2 DME5HIS Discovery agent N.A. Investigative [163]
Tyr-Pro-Hfe-Pro-NH2 DMJBR75 Discovery agent N.A. Investigative [163]
Tyr-Pro-Imp-Phe-NH2 DMUV3ZW Discovery agent N.A. Investigative [106]
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 DMI65GV Discovery agent N.A. Investigative [158]
Tyr-Pro-L-(NMe)Phe-Pro-NH2 DM1NITL Discovery agent N.A. Investigative [158]
Tyr-Pro-L-Phe-D-Pro-NH2 DMUVHGS Discovery agent N.A. Investigative [158]
Tyr-Pro-L-Phe-Pro-NH2 DM8VW3Z Discovery agent N.A. Investigative [158]
Tyr-Pro-Mmp-Phe-NH DMRE7G3 Discovery agent N.A. Investigative [106]
Tyr-Pro-Phe-Ala-Bn DMIE4U5 Discovery agent N.A. Investigative [164]
Tyr-Pro-Phe-D-2-Nal-NH2 DMLQ3PR Discovery agent N.A. Investigative [108]
Tyr-Pro-Phe-D-Ala-Bn DMLEUF6 Discovery agent N.A. Investigative [164]
Tyr-Pro-Phe-D-Phg-NH2 DM6YRVT Discovery agent N.A. Investigative [163]
Tyr-Pro-Phe-D-Val-Bn DM1QZ9X Discovery agent N.A. Investigative [164]
Tyr-Pro-Phe-Hfe-NH2 DM71P2O Discovery agent N.A. Investigative [163]
Tyr-Pro-Phe-Phe-N(CH3)2 DM5DRIZ Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-NHCH3 DM2U4VI Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-NHNH2 DMY6V9R Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-OC(CH3)3 DMS4P1E Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-OCH2CH3 DMZNHEC Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-OCH2OH DMFV7NI Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phe-OCH3 DMRQXHO Discovery agent N.A. Investigative [165]
Tyr-Pro-Phe-Phg-NH2 DM70HYT Discovery agent N.A. Investigative [163]
Tyr-Pro-Phg-Phe-NH2 DMVDM73 Discovery agent N.A. Investigative [163]
Tyr-Pro-Phg-Pro-NH2 DMSGMPU Discovery agent N.A. Investigative [163]
Tyr-Pro-Tmp-Phe-NH DMR3IVB Discovery agent N.A. Investigative [106]
Tyr-Pro-Trp-D-Ala-Bn DMFIPXA Discovery agent N.A. Investigative [164]
Tyr-Pro-Trp-D-Val-Bn DMY5HX6 Discovery agent N.A. Investigative [164]
Tyr-Pro-Trp-Gly-Bn DMKLDWF Discovery agent N.A. Investigative [164]
Tyr-Sar-Phe-D-2-Nal-NH2 DMIZB25 Discovery agent N.A. Investigative [108]
UFP-502 DMD8BRG Discovery agent N.A. Investigative [102]
UFP-512 DMYPVSJ Discovery agent N.A. Investigative [102]
YAWF-NH2 DMUW4KG Discovery agent N.A. Investigative [82]
YGGWL-NH2 DM5LYKW Discovery agent N.A. Investigative [82]
YGWFL-NH2 DMQ2EYJ Discovery agent N.A. Investigative [82]
YPAA-NH2 DMC3DK5 Discovery agent N.A. Investigative [82]
YPWA-NH2 DMOTHAC Discovery agent N.A. Investigative [82]
YRFB DMXOJIB Discovery agent N.A. Investigative [81]
ZYKLOPHIN DM0S5PE Discovery agent N.A. Investigative [135]
[3H]diprenorphine DMBMS1U Discovery agent N.A. Investigative [95]
[3H]U69593 DM6RSZ9 Discovery agent N.A. Investigative [90]
[D-Ala2]Met-enkephalinamide DM18ZNJ Discovery agent N.A. Investigative [146]
[Dcp1]Dyn A(1-11)-NH2 DM23GCK Discovery agent N.A. Investigative [100]
[Leu5]enkephalin DMA0N32 Discovery agent N.A. Investigative [166]
[Tyr-Pro-Phe-NH-CH2-]2 DMZTRQ0 Discovery agent N.A. Investigative [167]
[Tyr-Pro-Phe-NH-]2 DM61RG2 Discovery agent N.A. Investigative [167]
[Tyr-Pro-Phe-Phe-NH-CH2-]2 DMFGO4W Discovery agent N.A. Investigative [167]
[Tyr-Pro-Phe-Phe-NH-]2 DME6TNL Discovery agent N.A. Investigative [167]
------------------------------------------------------------------------------------
⏷ Show the Full List of 449 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Major depressive disorder 6A20 Pre-frontal cortex 5.94E-01 -0.02 -0.17
Asthma CA23 Nasal and bronchial airway 7.39E-01 3.94E-03 0.02
Lung cancer 2C82 Lung tissue 1.72E-01 0.02 0.11
Irritable bowel syndrome DD91.0 Rectal colon tissue 7.80E-01 0.09 0.31
------------------------------------------------------------------------------------

References

1 The pro-nociceptive effects of remifentanil or surgical injury in mice are associated with a decrease in delta-opioid receptor mRNA levels: Prevent... Pain. 2009 Jan;141(1-2):88-96.
2 Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87.
3 Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77.
4 Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
7 Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8.
8 Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
9 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
10 Clinical pipeline report, company report or official report of kempharm.
11 Clinical pipeline report, company report or official report of signaturerx.
12 Methadone-related opioid agonist pharmacotherapy for heroin addiction. History, recent molecular and neurochemical research and future in mainstream medicine. Ann N Y Acad Sci. 2000;909:186-216.
13 Acetylmethadol metabolites influence opiate receptors and adenylate cyclase in amygdala. Eur J Pharmacol. 1981 Jul 10;72(4):343-9.
14 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
15 Antianalgesia: stereoselective action of dextro-morphine over levo-morphine on glia in the mouse spinal cord.J Pharmacol Exp Ther.2005 Sep;314(3):1101-8.
16 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
17 Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
18 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
19 OxyContin abuse and overdose. Postgrad Med. 2009 Mar;121(2):163-7.
20 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 319).
21 Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents. Cardiovasc Res. 1999 Dec;44(3):568-78.
22 Cebranopadol: a first in-class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist. Br J Anaesth. 2015 Mar;114(3):364-6.
23 Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71.
24 A Review of Abuse-Deterrent Opioids For Chronic Nonmalignant Pain. P T. 2012 July; 37(7): 412-418.
25 Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94.
26 Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
27 Further studies of tyrosine surrogates in opioid receptor peptide ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60.
28 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
29 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
30 The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91.
31 Endomorphin-2: A Biased Agonist at the -Opioid Receptor. Mol Pharmacol. 2012 August; 82(2): 178-188.
32 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
33 US patent application no. 6,924,288, Enantiomerically pure opioid diarylmethylpiperzine and methods of using same.
34 Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists. J Med Chem. 2008 Feb 28;51(4):1058-62.
35 Herkinorin analogues with differential beta-arrestin-2 interactions. J Med Chem. 2008 Apr 24;51(8):2421-31.
36 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
37 Novel opioid antagonists for opioid-induced bowel dysfunction. Expert Opin Investig Drugs. 2011 Aug;20(8):1047-56.
38 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009073)
39 DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. II. A mixed opioid agonist with potent antinociceptive activity and limited effects on respiratory function. J Pharmacol Exp Ther. 2003 Dec;307(3):1227-33.
40 Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71.
41 A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo. Anesth Analg. 2005 Mar;100(3):713-7, table of contents.
42 Mirfentanil: pharmacological profile of a novel fentanyl derivative with opioid and nonopioid effects. J Pharmacol Exp Ther. 1991 Aug;258(2):502-10.
43 [3H]Sufentanil, a superior ligand for mu-opiate receptors: binding properties and regional distribution in rat brain and spinal cord. Eur J Pharmacol. 1983 Feb 18;87(2-3):209-25.
44 Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Clin Pharmacol Ther. 1994 Sep;56(3):261-71.
45 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026307)
46 WO patent application no. 2007,0677,14, Treatment of sequelae of psychiatric disorders.
47 Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
48 Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6.
49 Inhibition of cholinergic neurotransmission in human airways by opioids. J Appl Physiol (1985). 1992 Mar;72(3):1096-100.
50 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003724)
51 Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing tw... J Med Chem. 2010 Aug 12;53(15):5491-501.
52 The effects on resting ventilation of intravenous infusions of morphine or sameridine, a novel molecule with both local anesthetic and opioid properties. Anesth Analg. 1999 Jan;88(1):160-5.
53 Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5.
54 Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem. 2006 May 18;49(10):2868-75.
55 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
56 Akuammine and dihydroakuammine, two indolomonoterpene alkaloids displaying affinity for opioid receptors. J Nat Prod. 1992 Mar;55(3):380-4.
57 Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opio... J Med Chem. 2006 Jan 12;49(1):256-62.
58 6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides. J Med Chem. 2006 Jun 15;49(12):3653-8.
59 Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. J Med Chem. 2005 Dec 15;48(25):8035-44.
60 Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
61 Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
62 The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety. Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23.
63 Discovery of novel triazole-based opioid receptor antagonists. J Med Chem. 2006 Jul 13;49(14):4044-7.
64 14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. J Med Chem. 2009 Mar 26;52(6):1553-7.
65 Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors. J Med Chem. 2010 Jan 14;53(1):402-18.
66 Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorp... J Med Chem. 2006 Aug 24;49(17):5333-8.
67 Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic ... Bioorg Med Chem. 2009 Aug 15;17(16):5782-90.
68 3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8.
69 Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity. J Med Chem. 1992 May 1;35(9):1521-5.
70 Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM: Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. J Med Chem. 2000 Feb 10;43(3):381-91.
71 You HJ, Colpaert FC, Arendt-Nielsen L: The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes. Exp Neurol. 2005 Jan;191(1):174-83.
72 Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52.
73 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
74 Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) b... J Med Chem. 2009 Sep 24;52(18):5685-702.
75 Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-pipe... J Med Chem. 2008 Oct 9;51(19):5893-6.
76 Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. J Med Chem. 1981 Jul;24(7):903-6.
77 Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes. Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4.
78 SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10.
79 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-c... Bioorg Med Chem. 2008 May 15;16(10):5653-64.
80 Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50.
81 Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac... Bioorg Med Chem Lett. 2006 Sep 15;16(18):4839-41.
82 Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues. Bioorg Med Chem. 2008 Apr 15;16(8):4341-6.
83 Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4946-50.
84 Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp]. J Med Chem. 2008 Sep 25;51(18):5866-70.
85 Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.
86 Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture. J Neurochem. 1993 Feb;60(2):765-7.
87 Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. J Med Chem. 2009 Dec 10;52(23):7372-5.
88 Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine. J Med Chem. 1990 Aug;33(8):2286-96.
89 Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pha... J Med Chem. 2000 Jan 13;43(1):114-22.
90 Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5.
91 Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. J Med Chem. 2007 Nov 1;50(22):5528-32.
92 Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis. J Med Chem. 2007 Jun 28;50(13):3138-42.
93 Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. J Biol Chem. 2007 Sep 14;282(37):27126-32.
94 Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8.
95 Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. Mol Pharmacol. 1994 Feb;45(2):330-4.
96 Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonis... J Med Chem. 2004 Jun 3;47(12):3242-7.
97 Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors. J Med Chem. 1986 Nov;29(11):2370-5.
98 Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokini... J Med Chem. 2007 Jun 14;50(12):2779-86.
99 Evaluation of N-substitution in 6,7-benzomorphan compounds. Bioorg Med Chem. 2010 Jul 15;18(14):4975-82.
100 Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opio... J Med Chem. 2006 Aug 24;49(17):5382-5.
101 Synthesis and structure-activity relationships of deltorphin analogues. J Med Chem. 1991 May;34(5):1656-61.
102 Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds. Bioorg Med Chem. 2010 Aug 15;18(16):6024-30.
103 Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5.
104 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
105 [6-O-methyl-11C]Diprenorphine Molecular Imaging and Contrast Agent Database (MICAD) [Internet].
106 Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mi... J Med Chem. 2007 Jun 14;50(12):2753-66.
107 Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D... J Med Chem. 2007 Feb 8;50(3):512-20.
108 Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1350-3.
109 Peptides as receptor selectivity modulators of opiate pharmacophores. J Med Chem. 1986 Jul;29(7):1222-5.
110 Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3.
111 Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. Eur J Med Chem. 2010 Oct;45(10):4594-600.
112 Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4115-8.
113 Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. Br J Clin Pharmacol. 1995 Jun;39(6):611-20.
114 Ligand binding to nucleic acids and proteins: Does selectivity increase with strength Eur J Med Chem. 2008 Nov;43(11):2307-15.
115 Internalization of mu-opioid receptors produced by etorphine in the rat locus coeruleus. Neuroscience. 2001;108(3):467-77.
116 Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. Bioorg Med Chem. 2008 Mar 15;16(6):3218-23.
117 Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9.
118 Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1). J Med Chem. 2009 Nov 12;52(21):6941-5.
119 Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biologi... J Med Chem. 2000 Feb 24;43(4):569-80.
120 New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands. J Med Chem. 2006 Jun 29;49(13):3990-3.
121 From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. J Med Chem. 2005 Aug 25;48(17):5608-11.
122 Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists. J Med Chem. 2007 Jan 25;50(2):328-33.
123 Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic. J Med Chem. 2008 Aug 28;51(16):5109-17.
124 Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic. J Med Chem. 2004 Dec 16;47(26):6541-6.
125 Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore. J Med Chem. 2006 Sep 7;49(18):5610-7.
126 New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20.
127 Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502). Bioorg Med Chem. 2008 Mar 15;16(6):3032-8.
128 A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic. Bioorg Med Chem. 2007 Nov 15;15(22):6876-81.
129 Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity. J Med Chem. 2007 Mar 22;50(6):1414-7.
130 Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity. J Med Chem. 1991 Oct;34(10):3125-32.
131 Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. J Med Chem. 1993 Nov 26;36(24):3748-56.
132 A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid ... J Med Chem. 2008 Mar 13;51(5):1369-76.
133 Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. J Med Chem. 2006 Mar 9;49(5):1773-80.
134 Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. J Med Chem. 2007 Jan 11;50(1):165-8.
135 The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues. J Med Chem. 2009 Nov 12;52(21):6814-21.
136 Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide. J Med Chem. 1994 Sep 2;37(18):2856-64.
137 Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8.
138 Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1055-8.
139 Potential affinity labels for the opiate receptor based on fentanyl and related compounds. J Med Chem. 1982 Aug;25(8):913-9.
140 14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid rece... J Med Chem. 2009 Nov 12;52(21):6926-30.
141 Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands. J Med Chem. 2009 Dec 10;52(23):7389-96.
142 In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. Bioorg Med Chem. 2007 Jun 15;15(12):4106-12.
143 Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9.
144 High-affinity carbamate analogues of morphinan at opioid receptors. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11.
145 New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores. J Med Chem. 2006 Sep 7;49(18):5640-3.
146 Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates a... J Med Chem. 1982 Dec;25(12):1423-7.
147 Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers. J Med Chem. 1991 Aug;34(8):2438-44.
148 Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization. Bioorg Med Chem. 2007 Feb 15;15(4):1694-702.
149 Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4978-81.
150 Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5035-8.
151 Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an ... J Med Chem. 2007 Aug 9;50(16):3765-76.
152 Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility. J Med Chem. 2008 Apr 24;51(8):2571-4.
153 Respiratory effects and tolerability of Mr 2264 Cl.A new opiate partial agonist in comparison with morphine and placebo.Eur J Clin Pharmacol.1994;46(4):301-4.
154 Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selecti... J Med Chem. 1999 Dec 30;42(26):5359-68.
155 Design and synthesis of KNT-127, a -opioid receptor agonist effective by systemic administration. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5.
156 Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normo... Bioorg Med Chem. 2009 Aug 15;17(16):5983-8.
157 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
158 A topochemical approach to explain morphiceptin bioactivity. J Med Chem. 1993 Mar 19;36(6):708-19.
159 Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. J Med Chem. 2008 Jan 10;51(1):173-7.
160 The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokin... J Med Chem. 2008 Oct 23;51(20):6334-47.
161 Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. J Med Chem. 1997 Aug 29;40(18):2948-52.
162 Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. J Med Chem. 1994 Jan 7;37(1):141-5.
163 Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3... Bioorg Med Chem Lett. 2006 Jul 15;16(14):3688-92.
164 Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5387-91.
165 Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. Bioorg Med Chem. 2008 Jun 15;16(12):6415-22.
166 Carba-analogues of fentanyl are opioid receptor agonists. J Med Chem. 2010 Apr 8;53(7):2875-81.
167 Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1847-50.