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TRPV Cation Channels

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Definition: A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.      Other names Receptors, Vanilloid; Receptors, Capsaicin; Channels, TRPV Cation; Cation Channels, TRPV; Vanilloid Receptors; Capsaicin Receptors
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
TRPV4 protein, zebrafish  0   *Zebrafish Proteins *TRPV Cation Channels. Microsc Res Tech. 2012 Jan;75(1):89-96
4,5-diethyl-3-(2-methoxyethylthio)-2-methyl-6-phenyl-1,4-dihydropyridine-3,5-dicarboxylate  0   *Dihydropyridines TRPV Cation Channels/agonists. J Pharmacol Exp Ther. 2012 Jan;340(1):152-60
(2-(2,6-dichlorobenzyl)thiazolo(5,4-d)pyrimidin-7-yl)-(4-trifluoromethylphenyl)amine  0   *Pyrimidines *Thiazoles TRPV Cation Channels/antagonists & inhibitors. Eur J Pharmacol 2011 Aug 1;663(1-3):40-50
N-(1-(3,5-difluoro-4-methanesulfonylaminophenyl)ethyl)-3-(2-propyl-6-trifluoromethylpyridine-3-yl)acrylamide  0   *Acrylamides *Pyridines TRPV Cation Channels/antagonists & inhibitors. J Dermatol Sci 2011 Apr;62(1):8-15
4-tert-butylcyclohexanol  0   *Cyclohexanols TRPV Cation Channels/antagonists & inhibitors. Exp Dermatol 2010 Nov;19(11):980-6
N-(1-methyl-2-oxo-1,2,3,4-tetrahydro-7-quinolyl)-2-((2-methylpyrrolidin-1-yl)methyl)biphenyl-4-carboxamide  0   *Benzamides *Quinolones TRPV Cation Channels/antagonists & inhibitors. J Pharmacol Exp Ther 2011 Mar;336(3):743-50
2-(4-tert-butylbenzyl)-3-(2-(4-amino-3-bromo-5-methoxyphenyl)acetamido)propyl pivalate  0   *Benzamides TRPV Cation Channels/agonists. Bioorg Med Chem 2010 Nov 15;18(22):8092-105
2-(4-tert-butylbenzyl)-3-(2-(4-hydroxy-3-iodo-5-methoxyphenyl)acetamido)propyl pivalate  0   *Benzamides TRPV Cation Channels/agonists. Bioorg Med Chem 2010 Nov 15;18(22):8092-105
ABT 116  0   *Indazoles *Phenylurea Compounds TRPV Cation Channels. Bioorg Med Chem Lett 2010 Jun 1;20(11):3291-4
TRPV1 protein, Xenopus  0   *Xenopus Proteins *TRPV Cation Channels. Cell 2010 May 28;141(5):834-45
7-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)-1,8-naphthyridin-4-amine  0   *Naphthyridines TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2010 Apr 22;53(8):3330-48
RN 1734  0   *Sulfonamides TRPV Cation Channels/antagonists & inhibitors. Biochem Biophys Res Commun 2009 Nov 20;389(3):490-4
RN 1747  0   *Sulfonamides TRPV Cation Channels/agonists. Biochem Biophys Res Commun 2009 Nov 20;389(3):490-4
coniferyl 8-methylnonanoate  0   Capsaicin/*analogs & derivatives TRPV Cation Channels/agonists. Phytochemistry 2008 Mar;69(5):1179-84
coniferyl (E)-8-methyl-6-nonenoate  0   Capsaicin/*analogs & derivatives TRPV Cation Channels/agonists. Phytochemistry 2008 Mar;69(5):1179-84
4-methyl-N-oleoyldopamine  0   *Oleic Acids Dopamine/*analogs & derivatives TRPV Cation Channels/antagonists & inhibitors. Life Sci 2008 Mar 12;82(11-12):644-51
N-(2-(5-hydroxy-1H-indol-3-yl)ethyl)-(1,1'-biphenyl)-3-acetamide  0   *Biphenyl Compounds *Indoles TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Dec 27;50(26):6554-69
arginyl-(N-(2,4-dichlorophenethyl)glycyl)-N-(2-(indol-3-yl)ethyl)glycinamide  0   *Oligopeptides TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Nov 29;50(24):6133-43
N-(2-(4-t-butylbenzyl)-3-(pivaloyloxy)propyl)-2-(3-chloro-4-(methylsulfonylamino)phenyl)propionamide  0   *Mesylates *Benzeneacetamides TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2008 Jan 10;51(1):57-67
N-(2-(4-t-butylbenzyl)-3-(pivaloyloxy)propyl)-2-(3-fluoro-4-(methylsulfonylamino)phenyl)propionamide  0   *Mesylates *Benzeneacetamides TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2008 Jan 10;51(1):57-67
N-(3-trichloromethyl-4-(8-azabicyclo(3.2.1)octan-8-yl)benzyl)-N'-(indazol-4-yl)urea  0   *Indazoles Urea/*analogs & derivatives TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Jul 26;50(15):3651-60
N-(4-(6-(4-(1-(4-fluorophenyl)ethyl)piperazin-1-yl)pyrimidin-4-yloxy)benzo(d)thiazol-2-yl)acetamide  0   *Pyrimidines *Benzothiazoles TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Jul 26;50(15):3528-39
N-(4-(6-(4-trifluoromethylphenyl)pyrimidin-4-yloxy)benzothiazol-2-yl)acetamide  0   *Pyrimidines *Benzothiazoles TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Jul 26;50(15):3515-27
N-(6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yl)quinolin-7-amine  0   *Aminoquinolines *Pyrimidines TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Jul 26;50(15):3497-514
7-(6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yloxy)quinoline  0   *Pyrimidines *Quinolines TRPV Cation Channels/antagonists & inhibitors. J Med Chem 2007 Jul 26;50(15):3497-514
N-(4-tert-butylbenzyl)-N'-(4-hydroxy-2-bromo-3-iodo-5-methoxybenzyl)thiourea  0   Thiourea/*analogs & derivatives TRPV Cation Channels/antagonists & inhibitors. Bioorg Med Chem Lett 2007 Jan 1;17(1):214-9
N-(3-(tert-butylcarbonyloxy)-2-(3,4-dimethylbenzyl)propyl)-N'-(4-hydroxy-2,3-diiodo-5-methoxybenzyl)thiourea  0   Thiourea/*analogs & derivatives TRPV Cation Channels/antagonists & inhibitors. Bioorg Med Chem Lett 2007 Jan 1;17(1):214-9
SB 705498  0   *Pyrrolidines Urea/*analogs & derivatives TRPV Cation Channels/agonists. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91
TRPV3 protein, rat  0   *TRPV Cation Channels. J Neurophysiol 2005 Nov;94(5):3069-80
ECaC protein, zebrafish  0   *Zebrafish Proteins *TRPV Cation Channels. Am J Physiol Regul Integr Comp Physiol 2005 Oct;289(4):R1202-11
TRPV1 receptor  0   *TRPV Cation Channels.
TRPV1 protein, human  0   *TRPV Cation Channels.
Trpv1 protein, rat  0   *TRPV Cation Channels. Nature 1997 Oct 23;389(6653):816-24
TRPV1 protein, mouse  0   *TRPV Cation Channels. J Neurosci 2004 Jul 14;24(28):6410-5
Ecac1 protein, rat  0   *Calcium Channels *TRPV Cation Channels.
Trpv5 protein, mouse  0   *Calcium Channels *TRPV Cation Channels.
TRPV5 protein, human  0   *TRPV Cation Channels.
Trpv3 protein, mouse  0   *TRPV Cation Channels.
Trpv4 protein, rat  0   *TRPV Cation Channels Osmotic Pressure.
Trpv4 protein, mouse  0   *TRPV Cation Channels Osmotic Pressure.
Trpv2 protein, mouse  0   *Calcium Channels *TRPV Cation Channels.
Trpv2 protein, rat  0   *TRPV Cation Channels. Brain Res. 2003 Aug 8;980(2):293-6
TRPV3 protein, human  0   *TRPV Cation Channels. Science 2002 Jun 14;296(5575):2046-9
Trpv6 protein, mouse  0   *Calcium Channels *TRPV Cation Channels Receptors, Virus. Biochem Biophys Res Commun 2001 Dec 21;289(5):1287-94
SDZ 249-665  0   Capsaicin/*analogs & derivatives Urea/*analogs & derivatives TRPV Cation Channels/agonists. Pain 2001 Jan;89(2-3):229-35
TRPV6 protein, human  0   *Calcium Channels *TRPV Cation Channels. Am J Physiol Gastrointest Liver Physiol 2001 Feb;280(2):G285-90
TRPV4 protein, human  0   *TRPV Cation Channels Osmotic Pressure. Nat Cell Biol 2000 Oct;2(10):695-702
TRPV2 protein, human  0   *TRPV Cation Channels. Nat Cell Biol 1999 Jul;1(3):165-70
TRPV6 channel  0   *TRPV Cation Channels. J Biol Chem 1999 Aug 6;274(32):22739-46
vanilloid receptor subtype 1  0   *TRPV Cation Channels Nociceptors. Nature 1998 Apr 1;398(6726):436-41
ECaC protein, Oryctolagus cuniculus  0   *Calcium Channels *TRPV Cation Channels. Genomics. 2000 Jul 1;67(1):48-53; J Biol Chem 1999 Mar 26;274(13):8375-8
capsazepine  0   Capsaicin/*analogs & derivatives TRPV Cation Channels. Trends Neurosci 1991;14(7):265
resiniferatoxin  57444-62-9 6,7-deepoxy-6,7-didehydro-5-deoxy-21-dephenyl-21-(phenylmethyl)daphnetoxin 20-(3-hydroxy-5-methoxybenzeneacetate)  *Diterpenes Neurotoxins TRPV Cation Channels. Cancer Res 1980;40(5):1400
piperine  7780-20-3   *Alkaloids *Piperidines *Benzodioxoles *Polyunsaturated Alkamides Cytochrome P-450 Enzyme System/antagonists & inhibitors Piper nigrum TRPV Cation Channels.

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012

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