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Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats.
Lehto SG, Tamir R, Deng H, Klionsky L, Kuang R, Le A, Lee D, Louis JC, Magal E, Manning BH, Rubino J, Surapaneni S, Tamayo N, Wang T, Wang J, Wang J, Wang W, Youngblood B, Zhang M, Zhu D, Norman MH, Gavva NR. Lehto SG, et al. Among authors: surapaneni s. J Pharmacol Exp Ther. 2008 Jul;326(1):218-29. doi: 10.1124/jpet.107.132233. Epub 2008 Apr 17. J Pharmacol Exp Ther. 2008. PMID: 18420600
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: surapaneni s. 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: surapaneni s. J Med Chem. 2007 Jul 26;50(15):3528-39. doi: 10.1021/jm070191h. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585751
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: surapaneni s. 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
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: surapaneni s. J Med Chem. 2007 Jul 26;50(15):3515-27. doi: 10.1021/jm070190p. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585750
Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans.
Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, Jang GR, Kesslak JP, Ni L, Norman MH, Palluconi G, Rose MJ, Salfi M, Tan E, Romanovsky AA, Banfield C, Davar G. Gavva NR, et al. Among authors: surapaneni s. Pain. 2008 May;136(1-2):202-10. doi: 10.1016/j.pain.2008.01.024. Epub 2008 Mar 11. Pain. 2008. PMID: 18337008 Clinical Trial.
ABT-963 [2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one], a highly potent and selective disubstituted pyridazinone cyclooxgenase-2 inhibitor.
Harris RR, Black L, Surapaneni S, Kolasa T, Majest S, Namovic MT, Grayson G, Komater V, Wilcox D, King L, Marsh K, Jarvis MF, Nuss M, Nellans H, Pruesser L, Reinhart GA, Cox B, Jacobson P, Stewart A, Coghlan M, Carter G, Bell RL. Harris RR, et al. Among authors: surapaneni s. J Pharmacol Exp Ther. 2004 Dec;311(3):904-12. doi: 10.1124/jpet.104.070052. Epub 2004 Jul 26. J Pharmacol Exp Ther. 2004. PMID: 15277581
122 results