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Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Moreland RB, Brioni JD, Stewart AO. Matulenko MA, et al. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5095-8. doi: 10.1016/j.bmcl.2004.07.068. Bioorg Med Chem Lett. 2004. PMID: 15380206
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. J Med Chem. 2004 Apr 22;47(9):2348-55. doi: 10.1021/jm0305669. J Med Chem. 2004. PMID: 15084133
Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.
Brioni JD, Moreland RB, Cowart M, Hsieh GC, Stewart AO, Hedlund P, Donnelly-Roberts DL, Nakane M, Lynch JJ 3rd, Kolasa T, Polakowski JS, Osinski MA, Marsh K, Andersson KE, Sullivan JP. Brioni JD, et al. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6758-63. doi: 10.1073/pnas.0308292101. Epub 2004 Apr 15. Proc Natl Acad Sci U S A. 2004. PMID: 15087502 Free PMC article.
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
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
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. J Med Chem. 2006 Dec 14;49(25):7450-65. doi: 10.1021/jm060662k. J Med Chem. 2006. PMID: 17149874
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts DL, Jarvis MF, Carroll WA. Florjancic AS, et al. Among authors: donnelly roberts dl. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2089-92. doi: 10.1016/j.bmcl.2008.01.095. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18272366
81 results