• Acs Med Chem Lett · Jun 2015

    Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.

    • Qingwei Zhang, Zhiren Xia, Shailen Joshi, Victoria E Scott, and Michael F Jarvis.
    • Neuroscience Research, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064, United States.
    • Acs Med Chem Lett. 2015 Jun 11;6(6):641-4.

    AbstractThe discovery of a novel peripherally acting and selective Cav3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bioavailability. Modification of 4 to further improve ADME properties led to the discovery of ABT-639. Following oral administration, ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat.

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