Wolkenberg Scott E, Zhao Zhijian, Wisnoski David D, Leister William H, O'Brien Julie, Lemaire Wei, Williams David L, Jacobson Marlene A, Sur Cyrille, Kinney Gene G, Pettibone Doug J, Tiller Philip R, Smith Sheri, Gibson Christopher, Ma Bennett K, Polsky-Fisher Stacey L, Lindsley Craig W, Hartman George D
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1492-5. doi: 10.1016/j.bmcl.2009.01.015. Epub 2009 Jan 10.
Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed.
甘氨酸转运体1（GlyT1）是通过增强谷氨酸能NMDA受体来治疗精神分裂症的一个新靶点。本文讨论了具有改善药代动力学性质（包括口服生物利用度）的4,4-二取代哌啶类GlyT1抑制剂的发现。
