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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: mcdonald ha. 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.
Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature.
Reilly RM, McDonald HA, Puttfarcken PS, Joshi SK, Lewis L, Pai M, Franklin PH, Segreti JA, Neelands TR, Han P, Chen J, Mantyh PW, Ghilardi JR, Turner TM, Voight EA, Daanen JF, Schmidt RG, Gomtsyan A, Kort ME, Faltynek CR, Kym PR. Reilly RM, et al. Among authors: mcdonald ha. J Pharmacol Exp Ther. 2012 Aug;342(2):416-28. doi: 10.1124/jpet.111.190314. Epub 2012 May 8. J Pharmacol Exp Ther. 2012. PMID: 22570364
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: mcdonald ha. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR. Gomtsyan A, et al. Among authors: mcdonald ha. J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2. J Med Chem. 2016. PMID: 27077528
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. Among authors: mcdonald ha. 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.
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: mcdonald ha. 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
Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.
Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR. Chen J, et al. Among authors: mcdonald ha. Pain. 2011 May;152(5):1165-1172. doi: 10.1016/j.pain.2011.01.049. Epub 2011 Mar 12. Pain. 2011. PMID: 21402443
TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists.
Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, Marsh K, Bianchi B, McDonald H, Niforatos W, Neelands TR, Moreland RB, Decker MW, Lee CH, Sullivan JP, Faltynek CR. Cui M, et al. J Neurosci. 2006 Sep 13;26(37):9385-93. doi: 10.1523/JNEUROSCI.1246-06.2006. J Neurosci. 2006. PMID: 16971522 Free PMC article.
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.
El Kouhen R, Surowy CS, Bianchi BR, Neelands TR, McDonald HA, Niforatos W, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR. El Kouhen R, et al. Among authors: mcdonald ha. J Pharmacol Exp Ther. 2005 Jul;314(1):400-9. doi: 10.1124/jpet.105.084103. Epub 2005 Apr 18. J Pharmacol Exp Ther. 2005. PMID: 15837819
42 results