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Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Cowart M, Latshaw SP, Bhatia P, Daanen JF, Rohde J, Nelson SL, Patel M, Kolasa T, Nakane M, Uchic ME, Miller LN, Terranova MA, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino BR, Lynch JJ 3rd, Sullivan JP, Hsieh GC, Moreland RB, Brioni JD, Stewart AO. Cowart M, et al. J Med Chem. 2004 Jul 15;47(15):3853-64. doi: 10.1021/jm030505a. J Med Chem. 2004. PMID: 15239663
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. 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
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
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Stewart AO, Cowart MD, Moreland RB, Latshaw SP, Matulenko MA, Bhatia PA, Wang X, Daanen JF, Nelson SL, Terranova MA, Namovic MT, Donnelly-Roberts DL, Miller LN, Nakane M, Sullivan JP, Brioni JD. Stewart AO, et al. Among authors: bhatia pa. J Med Chem. 2004 Apr 22;47(9):2348-55. doi: 10.1021/jm0305669. J Med Chem. 2004. PMID: 15084133
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP. Altenbach RJ, et al. Among authors: bhatia pa. J Med Chem. 2004 Jun 3;47(12):3220-35. doi: 10.1021/jm030551a. J Med Chem. 2004. PMID: 15163201
Dopamine D4 receptor signaling in the rat paraventricular hypothalamic nucleus: Evidence of natural coupling involving immediate early gene induction and mitogen activated protein kinase phosphorylation.
Bitner RS, Nikkel AL, Otte S, Martino B, Barlow EH, Bhatia P, Stewart AO, Brioni JD, Decker MW, Moreland RB. Bitner RS, et al. Neuropharmacology. 2006 Apr;50(5):521-31. doi: 10.1016/j.neuropharm.2005.10.009. Epub 2005 Dec 1. Neuropharmacology. 2006. PMID: 16324724
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
Stewart AO, Bhatia PA, Martin JG, Summers JB, Rodriques KE, Martin MB, Holms JH, Moore JL, Craig RA, Kolasa T, Ratajczyk JD, Mazdiyasni H, Kerdesky FA, DeNinno SL, Maki RG, Bouska JB, Young PR, Lanni C, Bell RL, Carter GW, Brooks CD. Stewart AO, et al. Among authors: bhatia pa. J Med Chem. 1997 Jun 20;40(13):1955-68. doi: 10.1021/jm9700474. J Med Chem. 1997. PMID: 9207936
22 results