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Page 1
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Kolasa T, Matulenko MA, Hakeem AA, Patel MV, Mortell K, Bhatia P, Henry R, Nakane M, Hsieh GC, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino B, El Kouhen O, Marsh KC, Wetter JM, Moreland RB, Brioni JD, Stewart AO. Kolasa T, et al. J Med Chem. 2006 Aug 24;49(17):5093-109. doi: 10.1021/jm060279f. J Med Chem. 2006. PMID: 16913699
Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist.
El-Kouhen O, Lehto SG, Pan JB, Chang R, Baker SJ, Zhong C, Hollingsworth PR, Mikusa JP, Cronin EA, Chu KL, McGaraughty SP, Uchic ME, Miller LN, Rodell NM, Patel M, Bhatia P, Mezler M, Kolasa T, Zheng GZ, Fox GB, Stewart AO, Decker MW, Moreland RB, Brioni JD, Honore P. El-Kouhen O, et al. Br J Pharmacol. 2006 Nov;149(6):761-74. doi: 10.1038/sj.bjp.0706877. Epub 2006 Oct 3. Br J Pharmacol. 2006. PMID: 17016515 Free PMC article.
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Zheng GZ, Bhatia P, Kolasa T, Patel M, El Kouhen OF, Chang R, Uchic ME, Miller L, Baker S, Lehto SG, Honore P, Wetter JM, Marsh KC, Moreland RB, Brioni JD, Stewart AO. Zheng GZ, et al. Among authors: el kouhen of. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4936-40. doi: 10.1016/j.bmcl.2006.06.053. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16809035
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO. Patel MV, et al. Among authors: el kouhen of. J Med Chem. 2006 Dec 14;49(25):7450-65. doi: 10.1021/jm060662k. J Med Chem. 2006. PMID: 17149874
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Wang X, Kolasa T, El Kouhen OF, Chovan LE, Black-Shaefer CL, Wagenaar FL, Garton JA, Moreland RB, Honore P, Lau YY, Dandliker PJ, Brioni JD, Stewart AO. Wang X, et al. Among authors: el kouhen of. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4303-7. doi: 10.1016/j.bmcl.2007.05.028. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17532216
Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging.
Yao BB, Hsieh G, Daza AV, Fan Y, Grayson GK, Garrison TR, El Kouhen O, Hooker BA, Pai M, Wensink EJ, Salyers AK, Chandran P, Zhu CZ, Zhong C, Ryther K, Gallagher ME, Chin CL, Tovcimak AE, Hradil VP, Fox GB, Dart MJ, Honore P, Meyer MD. Yao BB, et al. J Pharmacol Exp Ther. 2009 Jan;328(1):141-51. doi: 10.1124/jpet.108.145011. Epub 2008 Oct 17. J Pharmacol Exp Ther. 2009. PMID: 18931146
15 results