Target General Infomation
Target ID
T83193
Former ID
TTDC00049
Target Name
Vanilloid receptor 1
Gene Name
TRPV1
Synonyms
Capsaicin receptor; OTRPC1; Osm-9-like TRP channel 1; TrpV1; Vanilloid receptor 1; Transient receptor potential cation channel subfamily V member 1; TRPV1
Target Type
Clinical Trial
Disease Acute or chronic pain [ICD9: 338,780; ICD10: R52, G89]
Acute migraine [ICD9: 346; ICD10: G43]
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Asthma [ICD10: J45]
Chronic pathological pain [ICD9: 338,780; ICD10: R52, G89]
Cough [ICD9: 786.2; ICD10: R05]
Diabetic neuropathy; Postherpetic neuralgia [ICD9: 053.19, 250, 250.6, 356.0, 356.8; ICD10: E11.21, G44.847, G53.0, G64, G90.0]
Esophagus sensitivity; Gastroesophageal reflux disease [ICD9:530, 140-229; ICD10: K20-K22, K21]
Musculoskeletal pain [ICD9: 338,780; ICD10: R52, G89]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Overactive bladder disorder; Pain [ICD9:188, 596.51, 338, 356.0, 356.8, 780; ICD10: C67, N32.81, G64, G90.0, R52, G89]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Can be activated by endogenous compounds, including 12- hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis (By similarity). Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractorystate. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel.
BioChemical Class
Transient receptor family
Target Validation
T83193
UniProt ID
Sequence
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
Drugs and Mode of Action
Drug(s) Capsaicin Drug Info Approved Neuropathic pain [522464], [539611]
DWP-05195 Drug Info Phase 2 Neuropathic pain [523840]
GRC-15300 Drug Info Phase 2 Pain [523675]
PAC-14028 Drug Info Phase 2 Atopic dermatitis [524628]
Resiniferatoxin Drug Info Phase 2 Neuropathic pain [536374], [539616]
XEN-D0501 Drug Info Phase 2 Overactive bladder disorder [524905]
ABT-102 Drug Info Phase 1 Chronic pathological pain [522601]
GRC-6211 Drug Info Phase 1 Asthma [548350]
JNJ-39439335 Drug Info Phase 1 Musculoskeletal pain [523962]
MR-1817 Drug Info Phase 1 Pain [522759]
PF-3864086 Drug Info Phase 1 Pain [522429]
PHE-377 Drug Info Phase 1 Pain [549036]
SAR-115740 Drug Info Phase 1 Pain [548480]
A-425619 Drug Info Preclinical Pain [467460], [548222]
AZD1386 Drug Info Discontinued in Phase 2 Esophagus sensitivity; Gastroesophageal reflux disease [542765], [548687]
DA-5018 Drug Info Discontinued in Phase 2 Diabetic neuropathy; Postherpetic neuralgia [536374]
JTS-653 Drug Info Discontinued in Phase 2 Overactive bladder disorder; Pain [548768]
NGD-8243 Drug Info Discontinued in Phase 2 Acute or chronic pain [548267]
Nuvanil Drug Info Discontinued in Phase 2 Pain [545482]
AMG-517 Drug Info Discontinued in Phase 1 Chronic pathological pain [467473], [548085]
SB-705498 Drug Info Discontinued in Phase 1 Acute migraine [467650], [548140]
AMG-8562 Drug Info Terminated Pain [547931]
BL-1872 Drug Info Terminated Pain [547404]
Inhibitor (5E,8E,11E,14E)-Icosa-5,8,11,14-tetraenal Drug Info [527623]
(E)-3-(4-tert-Butyl-phenyl)-N-phenyl-acrylamide Drug Info [527363]
(E)-Octadec-9-enal Drug Info [527623]
(R)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea Drug Info [528843]
(S)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea Drug Info [528843]
1,3-dibenzyl urea Drug Info [529279]
1-(4-Bromo-benzyl)-3-quinazolin-8-yl-urea Drug Info [527423]
1-(isoquinolin-5-yl)-3-(1-phenylpropyl)urea Drug Info [528843]
1-(isoquinolin-5-yl)-3-(4-morpholinobenzyl)urea Drug Info [528909]
1-benzhydryl-3-(isoquinolin-5-yl)urea Drug Info [528843]
2-(4-pentylphenyl)-N-(pyridin-3-yl)acetamide Drug Info [529389]
4-(3-methylpyridin-2-yl)-N-p-tolylbenzamide Drug Info [528334]
4-(butyl(methyl)amino)-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-(cyclohexylamino)-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-(hexyl(methyl)amino)-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-(methyl(nonyl)amino)-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-(methyl(octyl)amino)-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-butyl-N-(7-hydroxynaphthalen-1-yl)benzamide Drug Info [529389]
4-butyl-N-(isoquinolin-5-yl)benzamide Drug Info [529389]
4-butyl-N-(pyridin-3-yl)benzamide Drug Info [529389]
4-butyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-butyl-N-phenylbenzamide Drug Info [529389]
4-decyl-N-(pyridin-3-yl)benzamide Drug Info [529389]
4-heptyl-N-(pyridin-3-yl)benzamide Drug Info [529389]
4-heptyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-hexyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-nonyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-octyl-N-(pyridin-3-yl)benzamide Drug Info [529389]
4-octyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-pentyl-N-pyridin-3-yl benzamide Drug Info [529389]
4-propyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide Drug Info [527001]
4-tert-butyl-N-(quinolin-3-yl)benzamide Drug Info [529389]
6'-Iodononivamide Drug Info [531210]
A-795614 Drug Info [529652]
AMG-628 Drug Info [528915]
ATC-120 Drug Info [530533]
CAPSAZEPINE Drug Info [528825]
IODORESINIFERATOXIN Drug Info [529209]
JNJ-17203212 Drug Info [528825]
MK-056 Drug Info [530533]
N-(4-iodophenyl)-4-(trifluoromethoxy)benzamide Drug Info [529233]
N-(4-iodophenyl)-4-(trifluoromethyl)benzamide Drug Info [529233]
N-(4-tert-butylphenyl)-4-(pyridin-2-yl)benzamide Drug Info [528334]
N-methyl-4-pentyl-N-(pyridin-3-yl)benzamide Drug Info [529389]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]lauramide Drug Info [529162]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]linoleamide Drug Info [529162]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]undecanamide Drug Info [529162]
Pyrrolidin-1-yl-thiourea Drug Info [527001]
SB-782443 Drug Info [529708]
SC-0030 Drug Info [530533]
Activator 12S-HPETE Drug Info [525777]
15S-HPETE Drug Info [525777]
2-APB Drug Info [527108]
5S-HETE Drug Info [543861]
5S-HPETE Drug Info [525777]
arvanil Drug Info [527254]
diphenylboronic anhydride Drug Info [543861]
phenylacetylrinvanil Drug Info [527206]
PPAHV Drug Info [525987]
Resiniferatoxin Drug Info [536374]
[3H]resiniferatoxin Drug Info [543861]
Blocker (channel blocker) 5'-iodoresiniferatoxin Drug Info [543861]
6-iodo-nordihydrocapsaicin Drug Info [543861]
A778317 Drug Info [528966]
agatoxin 489 Drug Info [527878]
AMG 9810 Drug Info [527355]
NADA Drug Info [543861]
SB452533 Drug Info [543861]
[125I]resiniferatoxin Drug Info [525935]
[3H]A778317 Drug Info [528966]
Blocker A-425619 Drug Info [537396]
A-993610 Drug Info [537396]
ABT-102 Drug Info [537396]
AMG-517 Drug Info [536410], [537396]
AMG-8562 Drug Info [537396]
AMG-8563 Drug Info [537396]
AZD1386 Drug Info [550288]
BCTC Drug Info [537396]
NGD-8243 Drug Info [537396]
SB-705498 Drug Info [536410], [537396]
Antagonist ABT-116 Drug Info [543861]
ASP-8370 Drug Info [543861]
DWP-05195 Drug Info [549736]
GRC-15300 Drug Info [544145]
GRC-6211 Drug Info [529807]
JNJ-39439335 Drug Info [533205]
JTS-653 Drug Info [543861]
KJM429 Drug Info [535565]
KMJ-372 Drug Info [543861]
MR-1817 Drug Info [548951]
PAC-14028 Drug Info [531868]
PF-3864086 Drug Info [551974]
PHE-377 Drug Info [551503]
SAR-115740 Drug Info [551861]
TRPV1 antagonists Drug Info [543861]
Vanilloid VR1 receptor antagonists Drug Info [543861]
XEN-D0501 Drug Info [531517]
Modulator BL-1872 Drug Info [556264]
DA-5018 Drug Info [1572591]
NE-28345 Drug Info [1572605]
TRPV1 inhibitor (pain) Drug Info [1572605]
Agonist Capsaicin Drug Info [528612], [529267]
LASSBio-881 Drug Info [543861]
Nuvanil Drug Info [544118]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Inflammatory mediator regulation of TRP channels
NetPath Pathway IL2 Signaling Pathway
Pathway Interaction Database Trk receptor signaling mediated by the MAPK pathway
Trk receptor signaling mediated by PI3K and PLC-gamma
Reactome TRP channels
References
Ref 467460(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: 4117).
Ref 467473(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: 4129).
Ref 467650(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: 4311).
Ref 522429ClinicalTrials.gov (NCT00747058) A Study To Investigate The Safety, Toleration And Pharmacokinetics Of Single Oral Doses Of PF-03864086 In Healthy Male Subjects. U.S. National Institutes of Health.
Ref 522464ClinicalTrials.gov (NCT00771511) Cervical Capsaicin for Labor Induction and Pain Relief. U.S. National Institutes of Health.
Ref 522601ClinicalTrials.gov (NCT00854659) A Safety, Tolerability and Pharmacokinetic Study of ABT-102 in Healthy Subjects. U.S. National Institutes of Health.
Ref 522759ClinicalTrials.gov (NCT00960180) Study Evaluating Single Ascending Doses of MR1817. U.S. National Institutes of Health.
Ref 523675ClinicalTrials.gov (NCT01463397) Efficacy and Safety of SAR292833 Administration for 4 Weeks in Patients With Chronic Peripheral Neuropathic Pain. U.S. National Institutes of Health.
Ref 523840ClinicalTrials.gov (NCT01557010) Evaluate the Efficacy and Safety of DWP05195 in Subjects With Post-Herpetic Neuralgia. U.S. National Institutes of Health.
Ref 523962ClinicalTrials.gov (NCT01631487) A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of JNJ-39439335 in Healthy Japanese and Caucasian Adult Male Participants. U.S. National Institutes of Health.
Ref 524628ClinicalTrials.gov (NCT02052531) Efficacy and Safety Study of PAC-14028 Cream in Dermal Pruritus. U.S. National Institutes of Health.
Ref 524905ClinicalTrials.gov (NCT02233699) A Study to Assess the Efficacy of XEN-D0501 in Reducing the Cough Frequency in Patients With Chronic Idiopathic Cough. U.S. National Institutes of Health.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 539611(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: 2486).
Ref 539616(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: 2491).
Ref 542765(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: 7820).
Ref 545482Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003434)
Ref 547404Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015962)
Ref 547931Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020509)
Ref 548085Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021804)
Ref 548140Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022354)
Ref 548222Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023258)
Ref 548267Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023970)
Ref 548350Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024886)
Ref 548480Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025854)
Ref 548687Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027672)
Ref 548768Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028532)
Ref 549036Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031648)
Ref
Ref 525777Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances. Proc Natl Acad Sci U S A. 2000 May 23;97(11):6155-60.
Ref 525935Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist. Mol Pharmacol. 2001 Jan;59(1):9-15.
Ref 525987Pharmacological differences between the human and rat vanilloid receptor 1 (VR1). Br J Pharmacol. 2001 Mar;132(5):1084-94.
Ref 527001Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
Ref 5271082-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J Biol Chem. 2004 Aug 20;279(34):35741-8. Epub 2004 Jun 11.
Ref 527206Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential. J Pharmacol Exp Ther. 2005 Feb;312(2):561-70. Epub 2004 Sep 8.
Ref 527254Cloning and pharmacological characterization of mouse TRPV1. Neurosci Lett. 2004 Nov 3;370(1):55-60.
Ref 527355AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther. 2005 Apr;313(1):474-84. Epub 2004 Dec 22.
Ref 527363J Med Chem. 2005 Jan 13;48(1):71-90.Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Ref 527423J Med Chem. 2005 Feb 10;48(3):744-52.Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Ref 527623J Med Chem. 2005 Jul 14;48(14):4663-9.The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination.
Ref 527878An inhibitor of TRPV1 channels isolated from funnel Web spider venom. Biochemistry. 2005 Nov 29;44(47):15544-9.
Ref 528334Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25.From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Ref 528612Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71.
Ref 528825J Med Chem. 2007 May 31;50(11):2589-96. Epub 2007 May 10.The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
Ref 528843Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. Epub 2007 May 3.Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Ref 528909J Med Chem. 2007 Jul 26;50(15):3651-60. Epub 2007 Jun 21.In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Ref 528915J Med Chem. 2007 Jul 26;50(15):3528-39. Epub 2007 Jun 22.Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Ref 528966[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. Epub 2007 Jul 27.
Ref 529162J Med Chem. 2007 Dec 27;50(26):6554-69. Epub 2007 Nov 21.New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain.
Ref 529209J Med Chem. 2008 Jan 10;51(1):57-67. Epub 2007 Dec 12.Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
Ref 529233Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8. Epub 2007 Dec 10.Synthesis of benzamide derivatives as TRPV1 antagonists.
Ref 529267Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival. Clin J Pain. 2008 Feb;24(2):142-54.
Ref 529279Eur J Med Chem. 2009 Jan;44(1):432-6. Epub 2007 Dec 28.Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents.
Ref 529389Bioorg Med Chem Lett. 2008 Apr 15;18(8):2730-4. Epub 2008 Mar 5.N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).
Ref 529652Bioorg Med Chem. 2008 Sep 15;16(18):8516-25. Epub 2008 Aug 7.Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Ref 529708Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. Epub 2008 Aug 31.Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Ref 529807GRC-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.
Ref 530533Bioorg Med Chem. 2010 Jan 1;18(1):111-6. Epub 2009 Nov 10.Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.
Ref 531210Bioorg Med Chem. 2010 Nov 15;18(22):8092-105. Epub 2010 Sep 18.Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Ref 531517An 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.
Ref 531868Development 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.
Ref 533205Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem. 2015 May 14;58(9):3859-74.
Ref 535565High affinity antagonists of the vanilloid receptor. Mol Pharmacol. 2002 Oct;62(4):947-56.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536410The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov. 2007 May;6(5):357-72.
Ref 537396Analgesic potential of TRPV1 antagonists. Biochem Pharmacol. 2009 Aug 1;78(3):211-6. Epub 2009 Mar 5.
Ref 543861(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: 507).
Ref 544118TRPV1: ON THE ROAD TO PAIN RELIEF. Curr Mol Pharmacol. 2008 November; 1(3): 255-269.
Ref 544145The discovery and development of analgesics: new mechanisms, new modalities. J Clin Invest. 2010 November 1; 120(11): 3753-3759.
Ref 548951Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030745)
Ref 549736TRPV1 Antagonists as Analgesic Agents. The Open Pain Journal, 2013, 6, (Suppl 1: M11), 108-118 .
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 551503Clinical pipeline report, company report or official report of Pharmeste.
Ref 551861Clinical pipeline report, company report or official report of Sanofi.
Ref 551974Clinical pipeline report, company report or official report of pfizer.
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Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1572605The ChEMBL database in 2017.

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