General Information of Drug (ID: DM4ATCI)

Drug Name
CAPSAZEPINE Drug Info
Synonyms
capsazepine; 138977-28-3; capsazepin; N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide; UNII-LFW48MY844; N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide; CHEMBL391997; LFW48MY844; ST50826300; CHEBI:70773; N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2H-2-benzazepine-2-carbothioamide; N-(2-[4-chlorophenyl]ethyl)-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
2733484
ChEBI ID
CHEBI:70773
CAS Number
CAS 138977-28-3
TTD Drug ID
DM4ATCI

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
phorbol 12-myristate 13-acetate DMJWD62 Acute myeloid leukaemia 2A60 Phase 2 [5]
GSK2798745 DM7V96W Heart failure BD10-BD13 Phase 2 [6]
citric acid DM80YI7 Discovery agent N.A. Investigative [7]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide DMFC8Q4 Discovery agent N.A. Investigative [8]
Pyrrolidin-1-yl-thiourea DMYNZXC Discovery agent N.A. Investigative [8]
SC-0030 DMD2WEQ Discovery agent N.A. Investigative [9]
bisandrographolide DMRSKGC Discovery agent N.A. Investigative [10]
GSK1016790A DMDHZR1 Discovery agent N.A. Investigative [11]
GSK2193874 DMY2XV3 Discovery agent N.A. Investigative [12]
RN1734 DMA3ZXM Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capsaicin DMGMF6V Back pain ME84.Z Approved [14]
CNTX-4975 DMB4JPG Knee osteoarthritis FA01 Phase 3 [15]
XEN-D0501 DMG7PDY Overactive bladder GC50.0 Phase 2 [16]
Resiniferatoxin DMP62L5 Neuropathic pain 8E43.0 Phase 2 [17]
PAC-14028 DM3816P Atopic dermatitis EA80 Phase 2 [18]
GRC-15300 DMWXJSZ Pain MG30-MG3Z Phase 2 [19]
DWP-05195 DMQKU2F Neuropathic pain 8E43.0 Phase 2 [20]
SB-705498 DMRYHWI Rhinitis FA20 Phase 2 [21]
GRC-6211 DMZ0D3V Asthma CA23 Phase 1 [22]
ABT-102 DMJFWPR Chronic pain MG30 Phase 1 [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [23]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [24]
Etretinate DM2CZFA Keratosis ED56 Approved [25]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [26]
Methotrexate DM2TEOL Anterior urethra cancer Approved [27]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [30]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [31]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [32]
⏷ 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
Transient receptor potential cation channel V1 (TRPV1) TTMI6F5 TRPV1_HUMAN Inhibitor [2]
Transient receptor potential cation channel V4 (TRPV4) TTKP2SU TRPV4_HUMAN Inhibitor [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Interstitial collagenase (MMP1) OTI4I2V1 MMP1_HUMAN Gene/Protein Processing [4]

References

1 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. (Ligand id: 2461).
2 The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. J Med Chem. 2007 May 31;50(11):2589-96.
3 Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52.
4 Transient receptor potential vanilloid-1 mediates heat-shock-induced matrix metalloproteinase-1 expression in human epidermal keratinocytes. J Invest Dermatol. 2007 Oct;127(10):2328-35. doi: 10.1038/sj.jid.5700880. Epub 2007 May 17.
5 Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem. 2002 Apr 19;277(16):13569-77.
6 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
7 Impaired pressure sensation in mice lacking TRPV4. J Biol Chem. 2003 Jun 20;278(25):22664-8.
8 N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.
9 Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4389-93.
10 Bisandrographolide from Andrographis paniculata activates TRPV4 channels. J Biol Chem. 2006 Oct 6;281(40):29897-904.
11 N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.
12 An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.
13 Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.
14 Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71.
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
16 An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):921-31.
17 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
18 Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6.
19 The discovery and development of analgesics: new mechanisms, new modalities. J Clin Invest. 2010 November 1; 120(11): 3753-3759.
20 TRPV1 Antagonists as Analgesic Agents. The Open Pain Journal, 2013, 6, (Suppl 1: M11), 108-118 .
21 Analgesic potential of TRPV1 antagonists. Biochem Pharmacol. 2009 Aug 1;78(3):211-6.
22 GRC-6211, a new oral specific TRPV1 antagonist, decreases bladder overactivity and noxious bladder input in cystitis animal models. J Urol. 2009 Jan;181(1):379-86.
23 Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
24 Oxidative Stress-Protective and Anti-Melanogenic Effects of Loliolide and Ethanol Extract from Fresh Water Green Algae, Prasiola japonica. Int J Mol Sci. 2018 Sep 18;19(9):2825. doi: 10.3390/ijms19092825.
25 The effects of a novel synthetic retinoid, seletinoid G, on the expression of extracellular matrix proteins in aged human skin in vivo. Clin Chim Acta. 2005 Dec;362(1-2):161-9. doi: 10.1016/j.cccn.2005.06.016. Epub 2005 Aug 1.
26 Ciprofloxacin enhances the stimulation of matrix metalloproteinase 3 expression by interleukin-1beta in human tendon-derived cells. A potential mechanism of fluoroquinolone-induced tendinopathy. Arthritis Rheum. 2002 Nov;46(11):3034-40. doi: 10.1002/art.10617.
27 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
28 Simvastatin reduces MMP1 expression in human smooth muscle cells cultured on polymerized collagen by inhibiting Rac1 activation. Arterioscler Thromb Vasc Biol. 2007 May;27(5):1043-9. doi: 10.1161/ATVBAHA.107.139881. Epub 2007 Feb 15.
29 Quercetin inhibits matrix metalloproteinase-1 expression in human vascular endothelial cells through extracellular signal-regulated kinase. Arch Biochem Biophys. 2001 Jul 1;391(1):72-8. doi: 10.1006/abbi.2001.2402.
30 Rofecoxib regulates the expression of genes related to the matrix metalloproteinase pathway in humans: implication for the adverse effects of cyclooxygenase-2 inhibitors. Clin Pharmacol Ther. 2006 Apr;79(4):303-15. doi: 10.1016/j.clpt.2005.12.306.
31 Interaction between the aryl hydrocarbon receptor and retinoic acid pathways increases matrix metalloproteinase-1 expression in keratinocytes. J Biol Chem. 2004 Jun 11;279(24):25284-93. doi: 10.1074/jbc.M402168200. Epub 2004 Apr 9.
32 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.