Target General Infomation
Target ID
T39013
Former ID
TTDR00409
Target Name
Vanilloid receptor
Target Type
Research
Disease Cough [ICD9: 786.2; ICD10: R05]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Target Validation
T39013
Inhibitor 1,3-dibenzyl urea Drug Info [1]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide Drug Info [2]
6'-Iodononivamide Drug Info [3]
A-795614 Drug Info [4]
AMG-628 Drug Info [5]
ATC-120 Drug Info [6]
CAPSAZEPINE Drug Info [7]
IODORESINIFERATOXIN Drug Info [8]
JNJ-17203212 Drug Info [7]
MK-056 Drug Info [6]
N-(4-tert-butylphenyl)-4-(pyridin-2-yl)benzamide Drug Info [9]
Pyrrolidin-1-yl-thiourea Drug Info [2]
SC-0030 Drug Info [6]
References
REF 1Eur 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 2Bioorg 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 3Bioorg 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 4Bioorg 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 5J 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 6Bioorg 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 7J 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 8J 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 9Bioorg 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.

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