General Information of Drug (ID: DMQREP2)

Drug Name
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info
Synonyms
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2; CCK-Opioid Peptide, 12; CHEMBL408083; BDBM21142; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
11614928
TTD Drug ID
DMQREP2

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pentagastrin DMRCLZB Diagnostic imaging N.A. Approved [2]
Ceruletide DM2WE5K Caerulein stimulated gastric and pancreatic secretion 5A4Y Approved [3]
GASTRAZOLE DMO3ITF Duodenal ulcer DA63 Phase 3 [4]
Dexloxiglumide DM52HUD Pancreatic malfunction DC30-DC3Z Phase 2 [5]
Spiroglumide DM7NJWY Stomach disease DA43-DA4Y Phase 2 [6]
TT-223 DMCDMFP Type-1 diabetes 5A10 Phase 2 [7]
Z 360 DM2M80G Discovery agent N.A. Phase 2 [8]
S-0509 DM4KWEF Ulcerative colitis DD71 Phase 2 [9]
YF-476 DM54MAJ Stomach ulcer DA60.Z Phase 2 [10]
Itriglumide DM5UFRO Anxiety disorder 6B00-6B0Z Phase 2 [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexloxiglumide DM52HUD Pancreatic malfunction DC30-DC3Z Phase 2 [12]
proglumide DM4MF9V Influenza virus infection 1E30-1E32 Phase 2 [13]
Lintitript DMS5X94 Obesity 5B81 Discontinued in Phase 2 [14]
Tarazepide DMX6ZYE Gastrointestinal disease DE2Z Discontinued in Phase 2 [15]
GI 181771 DMIUFS4 Obesity 5B81 Discontinued in Phase 2 [16]
Pranazepide DMP43IR Pancreatic malfunction DC30-DC3Z Discontinued in Phase 2 [17]
CE-326597 DMXO49B Obesity 5B81 Discontinued in Phase 2 [18]
UCL-2000; butabindide DML51D0 Obesity 5B81 Discontinued in Phase 1 [19]
SSR-125180 DMSOBW2 Obesity 5B81 Discontinued in Phase 1 [20]
T-0632 DML4M5K Pancreatic malfunction DC30-DC3Z Discontinued in Phase 1 [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Opioid receptor mu (MOP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [22]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [23]
Hydromorphone DMHP21E Back pain ME84.Z Approved [24]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [25]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [26]
Alfentanil DMVO0UB Anaesthesia 9A78.6 Approved [27]
Naloxegol DML0B41 Opioid-induced constipation DB32.1 Approved [28]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [29]
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [30]
Oxycodone DMXLKHV Osteoarthritis FA00-FA05 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Codeine DMJX6ZG Allergic rhinitis CA08.0 Approved [32]
Hydromorphone DMHP21E Back pain ME84.Z Approved [33]
Loperamide DMOJZQ9 Diarrhea ME05.1 Approved [34]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [29]
Oxycodone DMXLKHV Osteoarthritis FA00-FA05 Approved [35]
Butorphanol DM5KYPJ Pain MG30-MG3Z Approved [32]
Carfentanil DM7ADGX N. A. N. A. Phase 2 [36]
Met-enkephalin DMSZFTP Pain MG30-MG3Z Phase 2 [37]
AZD-2327 DM8FZOG Anxiety disorder 6B00-6B0Z Phase 2 [38]
ADL-5747 DMMUPTN Pain MG30-MG3Z Phase 2 [39]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cholecystokinin receptor type A (CCKAR) TTCG0AL CCKAR_HUMAN Inhibitor [1]
Gastrin/cholecystokinin type B receptor (CCKBR) TTVFO0U GASR_HUMAN Inhibitor [1]
Opioid receptor delta (OPRD1) TT27RFC OPRD_HUMAN Inhibitor [1]
Opioid receptor mu (MOP) TTKWM86 OPRM_HUMAN Inhibitor [1]

References

1 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.
2 Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
3 Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
4 Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
5 Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
6 Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
7 The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
8 Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
9 Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
10 CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
11 Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.
12 Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
13 Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
14 A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
15 Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
16 Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
17 Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
18 Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
19 Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
20 US patent application no. 8,748,419, Antagonists.
21 Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
22 Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
23 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.
24 Clinical pipeline report, company report or official report of signaturerx.
25 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
26 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
27 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.
28 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
29 Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
30 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.
31 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).
32 Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16.
33 Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. J Med Chem. 2004 Mar 11;47(6):1400-12.
34 Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8.
35 Oxycodone: a pharmacological and clinical review. Clin Transl Oncol. 2007 May;9(5):298-307.
36 Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
37 Delta-opioid receptor agonists inhibit neuromuscular transmission in human colon. Eur J Pharmacol. 1994 Sep 1;262(1-2):33-9.
38 Preclinical pharmacology of AZD2327: a highly selective agonist of the delta-opioid receptor. J Pharmacol Exp Ther. 2011 Jul;338(1):195-204.
39 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: 317).