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Overcoming the genotoxicity of a pyrrolidine substituted arylindenopyrimidine as a potent dual adenosine A(2A)/A(1) antagonist by minimizing bioactivation to an iminium ion reactive intermediate.
Lim HK, Chen J, Sensenhauser C, Cook K, Preston R, Thomas T, Shook B, Jackson PF, Rassnick S, Rhodes K, Gopaul V, Salter R, Silva J, Evans DC. Lim HK, et al. Chem Res Toxicol. 2011 Jul 18;24(7):1012-30. doi: 10.1021/tx1004437. Epub 2011 Jun 28. Chem Res Toxicol. 2011. PMID: 21667953
Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease.
Shook BC, Rassnick S, Wallace N, Crooke J, Ault M, Chakravarty D, Barbay JK, Wang A, Powell MT, Leonard K, Alford V, Scannevin RH, Carroll K, Lampron L, Westover L, Lim HK, Russell R, Branum S, Wells KM, Damon S, Youells S, Li X, Beauchamp DA, Rhodes K, Jackson PF. Shook BC, et al. Among authors: lim hk. J Med Chem. 2012 Feb 9;55(3):1402-17. doi: 10.1021/jm201640m. Epub 2012 Jan 26. J Med Chem. 2012. PMID: 22239465
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