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Page 1
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: kym pr. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
Analgesic potential of TRPV3 antagonists.
Reilly RM, Kym PR. Reilly RM, et al. Among authors: kym pr. Curr Top Med Chem. 2011;11(17):2210-5. doi: 10.2174/156802611796904889. Curr Top Med Chem. 2011. PMID: 21671874 Review.
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: kym pr. 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
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: kym pr. 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
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Kym PR, Souers AJ, Campbell TJ, Lynch JK, Judd AS, Iyengar R, Vasudevan A, Gao J, Freeman JC, Wodka D, Mulhern M, Zhao G, Wagaw SH, Napier JJ, Brodjian S, Dayton BD, Reilly RM, Segreti JA, Fryer RM, Preusser LC, Reinhart GA, Hernandez L, Marsh KC, Sham HL, Collins CA, Polakowski JS. Kym PR, et al. J Med Chem. 2006 Apr 6;49(7):2339-52. doi: 10.1021/jm0512286. J Med Chem. 2006. PMID: 16570930
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Lynch JK, Freeman JC, Judd AS, Iyengar R, Mulhern M, Zhao G, Napier JJ, Wodka D, Brodjian S, Dayton BD, Falls D, Ogiela C, Reilly RM, Campbell TJ, Polakowski JS, Hernandez L, Marsh KC, Shapiro R, Knourek-Segel V, Droz B, Bush E, Brune M, Preusser LC, Fryer RM, Reinhart GA, Houseman K, Diaz G, Mikhail A, Limberis JT, Sham HL, Collins CA, Kym PR. Lynch JK, et al. Among authors: kym pr. J Med Chem. 2006 Nov 2;49(22):6569-84. doi: 10.1021/jm060683e. J Med Chem. 2006. PMID: 17064075
Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.
Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR. Honore P, et al. Among authors: kym pr. Pain. 2009 Mar;142(1-2):27-35. doi: 10.1016/j.pain.2008.11.004. Epub 2009 Jan 9. Pain. 2009. PMID: 19135797
Analgesic potential of TRPV1 antagonists.
Kym PR, Kort ME, Hutchins CW. Kym PR, et al. Biochem Pharmacol. 2009 Aug 1;78(3):211-6. doi: 10.1016/j.bcp.2009.02.014. Epub 2009 Mar 5. Biochem Pharmacol. 2009. PMID: 19481638
83 results