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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: bannon aw. J Med Chem. 2007 Jul 26;50(15):3515-27. doi: 10.1021/jm070190p. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585750
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
Gavva NR, Bannon AW, Hovland DN Jr, Lehto SG, Klionsky L, Surapaneni S, Immke DC, Henley C, Arik L, Bak A, Davis J, Ernst N, Hever G, Kuang R, Shi L, Tamir R, Wang J, Wang W, Zajic G, Zhu D, Norman MH, Louis JC, Magal E, Treanor JJ. Gavva NR, et al. Among authors: bannon aw. J Pharmacol Exp Ther. 2007 Oct;323(1):128-37. doi: 10.1124/jpet.107.125674. Epub 2007 Jul 25. J Pharmacol Exp Ther. 2007. PMID: 17652633
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: bannon aw. 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
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW. Fotsch C, et al. Among authors: bannon aw. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060. Bioorg Med Chem Lett. 2005. PMID: 15745810
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: bannon aw. J Med Chem. 2006 Jun 15;49(12):3719-42. doi: 10.1021/jm060065y. J Med Chem. 2006. PMID: 16759115
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: bannon aw. 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: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Wang HL, Katon J, Balan C, Bannon AW, Bernard C, Doherty EM, Dominguez C, Gavva NR, Gore V, Ma V, Nishimura N, Surapaneni S, Tang P, Tamir R, Thiel O, Treanor JJ, Norman MH. Wang HL, et al. Among authors: bannon aw. J Med Chem. 2007 Jul 26;50(15):3528-39. doi: 10.1021/jm070191h. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585751
Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors.
Steiner AA, Turek VF, Almeida MC, Burmeister JJ, Oliveira DL, Roberts JL, Bannon AW, Norman MH, Louis JC, Treanor JJ, Gavva NR, Romanovsky AA. Steiner AA, et al. Among authors: bannon aw. J Neurosci. 2007 Jul 11;27(28):7459-68. doi: 10.1523/JNEUROSCI.1483-07.2007. J Neurosci. 2007. PMID: 17626206 Free PMC article.
58 results