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Page 1
Targeting TRP channels: beyond TRPV1.
Gomtsyan A, Szallasi A. Gomtsyan A, et al. Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):387-8. doi: 10.1007/s00210-015-1089-2. Epub 2015 Feb 10. Naunyn Schmiedebergs Arch Pharmacol. 2015. PMID: 25662184 No abstract available.
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Schmidt RG, Bayburt EK, Latshaw SP, Koenig JR, Daanen JF, McDonald HA, Bianchi BR, Zhong C, Joshi S, Honore P, Marsh KC, Lee CH, Faltynek CR, Gomtsyan A. Schmidt RG, et al. Among authors: gomtsyan a. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1338-41. doi: 10.1016/j.bmcl.2011.01.056. Epub 2011 Jan 21. Bioorg Med Chem Lett. 2011. PMID: 21315587
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. Garami A, et al. Among authors: gomtsyan a. Acta Physiol (Oxf). 2018 Jul;223(3):e13038. doi: 10.1111/apha.13038. Epub 2018 Feb 16. Acta Physiol (Oxf). 2018. PMID: 29352512 Free PMC article.
Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME. Voight EA, et al. Among authors: gomtsyan ar. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Gomtsyan A, Bayburt EK, Keddy R, Turner SC, Jinkerson TK, Didomenico S, Perner RJ, Koenig JR, Drizin I, McDonald HA, Surowy CS, Honore P, Mikusa J, Marsh KC, Wetter JM, Faltynek CR, Lee CH. Gomtsyan A, et al. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. doi: 10.1016/j.bmcl.2007.04.105. Epub 2007 May 3. Bioorg Med Chem Lett. 2007. PMID: 17507218
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Drizin I, Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, DiDomenico S, Koenig JR, Turner SC, Jinkerson TK, Brown BS, Keddy RG, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter JM, Polakowski JS, Segreti JA, Jarvis MF, Faltynek CR, Lee CH. Drizin I, et al. Among authors: gomtsyan a. Bioorg Med Chem. 2006 Jul 15;14(14):4740-9. doi: 10.1016/j.bmc.2006.03.027. Epub 2006 Apr 18. Bioorg Med Chem. 2006. PMID: 16621571
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Bianchi BR, El Kouhen R, Neelands TR, Lee CH, Gomtsyan A, Raja SN, Vaidyanathan SN, Surber B, McDonald HA, Surowy CS, Faltynek CR, Moreland RB, Jarvis MF, Puttfarcken PS. Bianchi BR, et al. Among authors: gomtsyan a. J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. doi: 10.1124/jpet.107.124305. Epub 2007 Jul 27. J Pharmacol Exp Ther. 2007. PMID: 17660385
TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats.
Gomtsyan A, McDonald HA, Schmidt RG, Daanen JF, Voight EA, Segreti JA, Puttfarcken PS, Reilly RM, Kort ME, Dart MJ, Kym PR. Gomtsyan A, et al. Temperature (Austin). 2015 May 22;2(2):297-301. doi: 10.1080/23328940.2015.1046013. eCollection 2015 Apr-Jun. Temperature (Austin). 2015. PMID: 27227030 Free PMC article.
36 results