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Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Ognyanov VI, Balan C, Bannon AW, Bo Y, Dominguez C, Fotsch C, Gore VK, Klionsky L, Ma VV, Qian YX, Tamir R, Wang X, Xi N, Xu S, Zhu D, Gavva NR, Treanor JJ, Norman MH. Ognyanov VI, et al. Among authors: treanor jj. J Med Chem. 2006 Jun 15;49(12):3719-42. doi: 10.1021/jm060065y. J Med Chem. 2006. PMID: 16759115
Molecular determinants of vanilloid sensitivity in TRPV1.
Gavva NR, Klionsky L, Qu Y, Shi L, Tamir R, Edenson S, Zhang TJ, Viswanadhan VN, Toth A, Pearce LV, Vanderah TW, Porreca F, Blumberg PM, Lile J, Sun Y, Wild K, Louis JC, Treanor JJ. Gavva NR, et al. Among authors: treanor jj. J Biol Chem. 2004 May 7;279(19):20283-95. doi: 10.1074/jbc.M312577200. Epub 2004 Mar 2. J Biol Chem. 2004. PMID: 14996838 Free article.
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.
Gavva NR, Tamir R, Qu Y, Klionsky L, Zhang TJ, Immke D, Wang J, Zhu D, Vanderah TW, Porreca F, Doherty EM, Norman MH, Wild KD, Bannon AW, Louis JC, Treanor JJ. Gavva NR, et al. Among authors: treanor jj. J Pharmacol Exp Ther. 2005 Apr;313(1):474-84. doi: 10.1124/jpet.104.079855. Epub 2004 Dec 22. J Pharmacol Exp Ther. 2005. PMID: 15615864
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.
Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC. Gavva NR, et al. Among authors: treanor jj. J Neurosci. 2007 Mar 28;27(13):3366-74. doi: 10.1523/JNEUROSCI.4833-06.2007. J Neurosci. 2007. PMID: 17392452 Free PMC article.
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R, Zhu J, Treanor JJ, Norman MH. Doherty EM, et al. Among authors: treanor jj. J Med Chem. 2007 Jul 26;50(15):3515-27. doi: 10.1021/jm070190p. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585750
216 results