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Items: 49


Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.

Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR.

J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10.


TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds' pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development.

Garami A, Pakai E, McDonald HA, Reilly RM, Gomtsyan A, Corrigan JJ, Pinter E, Zhu DXD, Lehto SG, Gavva NR, Kym PR, Romanovsky AA.

Acta Physiol (Oxf). 2018 Jul;223(3):e13038. doi: 10.1111/apha.13038. Epub 2018 Feb 16.


Selective antagonism of TRPA1 produces limited efficacy in models of inflammatory- and neuropathic-induced mechanical hypersensitivity in rats.

Lehto SG, Weyer AD, Youngblood BD, Zhang M, Yin R, Wang W, Teffera Y, Cooke M, Stucky CL, Schenkel L, Geuns-Meyer S, Moyer BD, Wild KD, Gavva NR.

Mol Pain. 2016 Nov 29;12. pii: 1744806916677761. Print 2016.


Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S.

J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4.


AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.

Lehto SG, Weyer AD, Zhang M, Youngblood BD, Wang J, Wang W, Kerstein PC, Davis C, Wild KD, Stucky CL, Gavva NR.

Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76. doi: 10.1007/s00210-015-1090-9. Epub 2015 Feb 10.


Antibodies to the extracellular pore loop of TRPM8 act as antagonists of channel activation.

Miller S, Rao S, Wang W, Liu H, Wang J, Gavva NR.

PLoS One. 2014 Sep 9;9(9):e107151. doi: 10.1371/journal.pone.0107151. eCollection 2014.


Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.

Copeland KW, Boezio AA, Cheung E, Lee J, Olivieri P, Schenkel LB, Wan Q, Wang W, Wells MC, Youngblood B, Gavva NR, Lehto SG, Geuns-Meyer S.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3464-8. doi: 10.1016/j.bmcl.2014.05.069. Epub 2014 Jun 6.


Mouse monoclonal antibodies to transient receptor potential ankyrin 1 act as antagonists of multiple modes of channel activation.

Lee KJ, Wang W, Padaki R, Bi V, Plewa CA, Gavva NR.

J Pharmacol Exp Ther. 2014 Aug;350(2):223-31. doi: 10.1124/jpet.114.215574. Epub 2014 Jun 3.


Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents.

de Oliveira C, Garami A, Lehto SG, Pakai E, Tekus V, Pohoczky K, Youngblood BD, Wang W, Kort ME, Kym PR, Pinter E, Gavva NR, Romanovsky AA.

J Neurosci. 2014 Mar 26;34(13):4445-52. doi: 10.1523/JNEUROSCI.5387-13.2014.


Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.

Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH.

J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19.


Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation.

Gavva NR, Davis C, Lehto SG, Rao S, Wang W, Zhu DX.

Mol Pain. 2012 May 9;8:36. doi: 10.1186/1744-8069-8-36.


Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.

Tamayo NA, Bo Y, Gore V, Ma V, Nishimura N, Tang P, Deng H, Klionsky L, Lehto SG, Wang W, Youngblood B, Chen J, Correll TL, Bartberger MD, Gavva NR, Norman MH.

J Med Chem. 2012 Feb 23;55(4):1593-611. doi: 10.1021/jm2013634. Epub 2012 Feb 13.


Pharmacological blockade of the cold receptor TRPM8 attenuates autonomic and behavioral cold defenses and decreases deep body temperature.

Almeida MC, Hew-Butler T, Soriano RN, Rao S, Wang W, Wang J, Tamayo N, Oliveira DL, Nucci TB, Aryal P, Garami A, Bautista D, Gavva NR, Romanovsky AA.

J Neurosci. 2012 Feb 8;32(6):2086-99. doi: 10.1523/JNEUROSCI.5606-11.2012.


Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory.

Wanner SP, Garami A, Pakai E, Oliveira DL, Gavva NR, Coimbra CC, Romanovsky AA.

Cell Cycle. 2012 Jan 15;11(2):343-9. doi: 10.4161/cc.11.2.18772. Epub 2012 Jan 15.


The hypothermic response to bacterial lipopolysaccharide critically depends on brain CB1, but not CB2 or TRPV1, receptors.

Steiner AA, Molchanova AY, Dogan MD, Patel S, Pétervári E, Balaskó M, Wanner SP, Eales J, Oliveira DL, Gavva NR, Almeida MC, Székely M, Romanovsky AA.

J Physiol. 2011 May 1;589(Pt 9):2415-31. doi: 10.1113/jphysiol.2010.202465. Epub 2011 Mar 14.


Thermoregulatory phenotype of the Trpv1 knockout mouse: thermoeffector dysbalance with hyperkinesis.

Garami A, Pakai E, Oliveira DL, Steiner AA, Wanner SP, Almeida MC, Lesnikov VA, Gavva NR, Romanovsky AA.

J Neurosci. 2011 Feb 2;31(5):1721-33. doi: 10.1523/JNEUROSCI.4671-10.2011.


Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia.

Garami A, Shimansky YP, Pakai E, Oliveira DL, Gavva NR, Romanovsky AA.

J Neurosci. 2010 Jan 27;30(4):1435-40. doi: 10.1523/JNEUROSCI.5150-09.2010.


Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks.

Wong GY, Gavva NR.

Brain Res Rev. 2009 Apr;60(1):267-77. doi: 10.1016/j.brainresrev.2008.12.006. Epub 2008 Dec 25. Review.


Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1.

Gavva NR.

Trends Pharmacol Sci. 2008 Nov;29(11):550-7. doi: 10.1016/ Epub 2008 Sep 19. Review.


Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.

Stec MM, Bo Y, Chakrabarti PP, Liao L, Ncube M, Tamayo N, Tamir R, Gavva NR, Treanor JJ, Norman MH.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5118-22. doi: 10.1016/j.bmcl.2008.07.112. Epub 2008 Jul 31.


Effect of AMG0347, a transient receptor potential type V1 receptor antagonist, and morphine on pain behavior after plantar incision.

Wu C, Gavva NR, Brennan TJ.

Anesthesiology. 2008 Jun;108(6):1100-8. doi: 10.1097/ALN.0b013e31817302b3.


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.

J Pharmacol Exp Ther. 2008 Jul;326(1):218-29. doi: 10.1124/jpet.107.132233. Epub 2008 Apr 17. Erratum in: J Pharmacol Exp Ther. 2008 Sep;326(3):999.


Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.

Tamayo N, Liao H, Stec MM, Wang X, Chakrabarti P, Retz D, Doherty EM, Surapaneni S, Tamir R, Bannon AW, Gavva NR, Norman MH.

J Med Chem. 2008 May 8;51(9):2744-57. doi: 10.1021/jm7014638. Epub 2008 Apr 3.


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.

Pain. 2008 May;136(1-2):202-10. doi: 10.1016/j.pain.2008.01.024. Epub 2008 Mar 11.


4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.

Doherty EM, Retz D, Gavva NR, Tamir R, Treanor JJ, Norman MH.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1830-4. doi: 10.1016/j.bmcl.2008.02.022. Epub 2008 Feb 13.


The vanilloid receptor TRPV1 is activated and sensitized by local anesthetics in rodent sensory neurons.

Leffler A, Fischer MJ, Rehner D, Kienel S, Kistner K, Sauer SK, Gavva NR, Reeh PW, Nau C.

J Clin Invest. 2008 Feb;118(2):763-76. doi: 10.1172/JCI32751.


Species-specific pharmacology of Trichloro(sulfanyl)ethyl benzamides as transient receptor potential ankyrin 1 (TRPA1) antagonists.

Klionsky L, Tamir R, Gao B, Wang W, Immke DC, Nishimura N, Gavva NR.

Mol Pain. 2007 Dec 17;3:39.


Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.

Wang X, Chakrabarti PP, Ognyanov VI, Pettus LH, Tamir R, Tan H, Tang P, Treanor JJ, Gavva NR, Norman MH.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6539-45. Epub 2007 Oct 15.


Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.

Gore VK, Ma VV, Tamir R, Gavva NR, Treanor JJ, Norman MH.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5825-30. Epub 2007 Aug 25.


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.

J Pharmacol Exp Ther. 2007 Oct;323(1):128-37. Epub 2007 Jul 25.


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.

J Neurosci. 2007 Jul 11;27(28):7459-68.


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.

J Med Chem. 2007 Jul 26;50(15):3528-39. Epub 2007 Jun 22.


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.

J Med Chem. 2007 Jul 26;50(15):3515-27. Epub 2007 Jun 22.


Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.

Norman MH, Zhu J, Fotsch C, Bo Y, Chen N, Chakrabarti P, Doherty EM, Gavva NR, Nishimura N, Nixey T, Ognyanov VI, Rzasa RM, Stec M, Surapaneni S, Tamir R, Viswanadhan VN, Treanor JJ.

J Med Chem. 2007 Jul 26;50(15):3497-514. Epub 2007 Jun 22.


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.

J Neurosci. 2007 Mar 28;27(13):3366-74.


The TRPV1 receptor and nociception.

Immke DC, Gavva NR.

Semin Cell Dev Biol. 2006 Oct;17(5):582-91. Epub 2006 Sep 24. Review.


A polyclonal antibody to the prepore loop of transient receptor potential vanilloid type 1 blocks channel activation.

Klionsky L, Tamir R, Holzinger B, Bi X, Talvenheimo J, Kim H, Martin F, Louis JC, Treanor JJ, Gavva NR.

J Pharmacol Exp Ther. 2006 Oct;319(1):192-8. Epub 2006 Jul 14.


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.

J Med Chem. 2006 Jun 15;49(12):3719-42.


Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.

Xi N, Bo Y, Doherty EM, Fotsch C, Gavva NR, Han N, Hungate RW, Klionsky L, Liu Q, Tamir R, Xu S, Treanor JJ, Norman MH.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5211-7. Epub 2005 Oct 3.


Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1.

Gavva NR, Tamir R, Klionsky L, Norman MH, Louis JC, Wild KD, Treanor JJ.

Mol Pharmacol. 2005 Dec;68(6):1524-33. Epub 2005 Aug 31.


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.

J Pharmacol Exp Ther. 2005 Apr;313(1):474-84. Epub 2004 Dec 22.


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.

J Biol Chem. 2004 May 7;279(19):20283-95. Epub 2004 Mar 2.


Gene expression analysis of spontaneously hypertensive rat cerebral cortex following transient focal cerebral ischemia.

Raghavendra Rao VL, Bowen KK, Dhodda VK, Song G, Franklin JL, Gavva NR, Dempsey RJ.

J Neurochem. 2002 Dec;83(5):1072-86.


NAPP2, a peroxisomal membrane protein, is also a transcriptional corepressor.

Gavva NR, Wen SC, Daftari P, Moniwa M, Yang WM, Yang-Feng LP, Seto E, Davie JR, Shen CK.

Genomics. 2002 Mar;79(3):423-31.


Human ITCH is a coregulator of the hematopoietic transcription factor NF-E2.

Chen X, Wen S, Fukuda MN, Gavva NR, Hsu D, Akama TO, Yang-Feng T, Shen CK.

Genomics. 2001 Apr 15;73(2):238-41.


Loading of DNA-binding factors to an erythroid enhancer.

Wen SC, Roder K, Hu KY, Rombel I, Gavva NR, Daftari P, Kuo YY, Wang C, Shen CK.

Mol Cell Biol. 2000 Mar;20(6):1993-2003.


Derepression of human embryonic zeta-globin promoter by a locus-control region sequence.

Huang BL, Fan-Chiang IR, Wen SC, Koo HC, Kao WY, Gavva NR, Shen CK.

Proc Natl Acad Sci U S A. 1998 Dec 8;95(25):14669-74.


Interaction of WW domains with hematopoietic transcription factor p45/NF-E2 and RNA polymerase II.

Gavva NR, Gavva R, Ermekova K, Sudol M, Shen CJ.

J Biol Chem. 1997 Sep 26;272(39):24105-8.

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