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新型甘氨酸转运体1(GlyT1)抑制剂的发现与构效关系研究

Discovery and SAR studies of novel GlyT1 inhibitors.

作者信息

Walter Magnus W, Hoffman Beth J, Gordon Kimberly, Johnson Kirk, Love Patrick, Jones Matthew, Man Teresa, Phebus Lee, Reel Jon K, Rudyk Helene C, Shannon Harlan, Svensson Kjell, Yu Hong, Valli Matthew J, Porter Warren J

机构信息

Lilly Research Laboratories, Eli Lilly and Company, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK.

出版信息

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5233-8. doi: 10.1016/j.bmcl.2007.06.074. Epub 2007 Jun 30.

Abstract

Inhibition of the glycine transporter GlyT1 is a potential strategy for the treatment of schizophrenia. A novel series of GlyT1 inhibitors and their structure-activity relationships (SAR) are described. Members of this series are highly potent and selective transport inhibitors which are shown to elevate glycine levels in cerebrospinal fluid.

摘要

抑制甘氨酸转运体GlyT1是治疗精神分裂症的一种潜在策略。本文描述了一系列新型的GlyT1抑制剂及其构效关系(SAR)。该系列成员是高效且具有选择性的转运抑制剂,已证明可提高脑脊液中的甘氨酸水平。

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