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Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, Didomenico S, Koenig JR, Turner S, Jinkerson T, Drizin I, Hannick SM, Macri BS, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter J, Stewart KD, Oie T, Jarvis MF, Surowy CS, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: honore p. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
Discovery of TRPV1 antagonist ABT-116.
Brown BS, Keddy R, Perner RJ, DiDomenico S, Koenig JR, Jinkerson TK, Hannick SM, McDonald HA, Bianchi BR, Honore P, Puttfarcken PS, Moreland RB, Marsh KC, Faltynek CR, Lee CH. Brown BS, et al. Among authors: honore p. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047. Epub 2010 Apr 14. Bioorg Med Chem Lett. 2010. PMID: 20457518
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE. Kort ME, et al. Among authors: honore p. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855211
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Altenbach RJ, Black LA, Strakhova MI, Manelli AM, Carr TL, Marsh KC, Wetter JM, Wensink EJ, Hsieh GC, Honore P, Garrison TR, Brioni JD, Cowart MD. Altenbach RJ, et al. Among authors: honore p. J Med Chem. 2010 Nov 11;53(21):7869-73. doi: 10.1021/jm100666w. J Med Chem. 2010. PMID: 20945906
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME. Scanio MJ, et al. Among authors: honore p. Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29. Bioorg Med Chem. 2010. PMID: 20965738
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: honore p. 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
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats.
Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. Honore P, et al. J Pharmacol Exp Ther. 2005 Jul;314(1):410-21. doi: 10.1124/jpet.105.083915. Epub 2005 Apr 18. J Pharmacol Exp Ther. 2005. PMID: 15837818
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: honore p. 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
950 results