Target Information
Target General Infomation | |||||
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Target ID |
T83193
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Former ID |
TTDC00049
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Target Name |
Vanilloid receptor 1
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Gene Name |
TRPV1
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Synonyms |
Capsaicin receptor; OTRPC1; Osm-9-like TRP channel 1; TrpV1; Vanilloid receptor 1; Transient receptor potential cation channel subfamily V member 1; TRPV1
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Target Type |
Clinical Trial
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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 [ICD9: 188, 596.51; ICD10: C67, N32.81] | |||||
Overactive bladder disorder; Pain [ICD9:188, 596.51, 338, 356.0, 356.8, 780; ICD10: C67, N32.81, G64, G90.0, R52, G89] | |||||
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.
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BioChemical Class |
Transient receptor family
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Target Validation |
T83193
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UniProt ID | |||||
Sequence |
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK |
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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 522429 | ClinicalTrials.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 522464 | ClinicalTrials.gov (NCT00771511) Cervical Capsaicin for Labor Induction and Pain Relief. U.S. National Institutes of Health. | ||||
Ref 522601 | ClinicalTrials.gov (NCT00854659) A Safety, Tolerability and Pharmacokinetic Study of ABT-102 in Healthy Subjects. U.S. National Institutes of Health. | ||||
Ref 522759 | ClinicalTrials.gov (NCT00960180) Study Evaluating Single Ascending Doses of MR1817. U.S. National Institutes of Health. | ||||
Ref 523675 | ClinicalTrials.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 523840 | ClinicalTrials.gov (NCT01557010) Evaluate the Efficacy and Safety of DWP05195 in Subjects With Post-Herpetic Neuralgia. U.S. National Institutes of Health. | ||||
Ref 523962 | ClinicalTrials.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 524628 | ClinicalTrials.gov (NCT02052531) Efficacy and Safety Study of PAC-14028 Cream in Dermal Pruritus. U.S. National Institutes of Health. | ||||
Ref 524905 | ClinicalTrials.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 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 545482 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003434) | ||||
Ref 547404 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015962) | ||||
Ref 547931 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020509) | ||||
Ref 548085 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021804) | ||||
Ref 548140 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022354) | ||||
Ref 548222 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023258) | ||||
Ref 548267 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023970) | ||||
Ref 548350 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024886) | ||||
Ref 548480 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025854) | ||||
Ref 548687 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027672) | ||||
Ref 525777 | Direct 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 525935 | Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist. Mol Pharmacol. 2001 Jan;59(1):9-15. | ||||
Ref 525987 | Pharmacological differences between the human and rat vanilloid receptor 1 (VR1). Br J Pharmacol. 2001 Mar;132(5):1084-94. | ||||
Ref 527001 | Bioorg 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 527108 | 2-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 527206 | Development 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 527254 | Cloning and pharmacological characterization of mouse TRPV1. Neurosci Lett. 2004 Nov 3;370(1):55-60. | ||||
Ref 527355 | AMG 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 527363 | J 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 527423 | J 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 527623 | J 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 527878 | An inhibitor of TRPV1 channels isolated from funnel Web spider venom. Biochemistry. 2005 Nov 29;44(47):15544-9. | ||||
Ref 528334 | Bioorg 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 528612 | Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71. | ||||
Ref 528825 | J 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 528843 | Bioorg 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 528909 | J 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 528915 | J 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 529162 | J 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 529209 | J 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 529233 | Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8. Epub 2007 Dec 10.Synthesis of benzamide derivatives as TRPV1 antagonists. | ||||
Ref 529267 | Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival. Clin J Pain. 2008 Feb;24(2):142-54. | ||||
Ref 529279 | Eur 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 529389 | Bioorg 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 529652 | Bioorg 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 529708 | Bioorg 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 529807 | 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. | ||||
Ref 530533 | Bioorg 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 531210 | Bioorg 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 531517 | 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. | ||||
Ref 531868 | 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. | ||||
Ref 533205 | Benzo[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. | ||||
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