鉴定结构新颖、选择性高、口服生物利用度好的 mGluR2 正向变构调节剂。
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
机构信息
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):759-62. doi: 10.1016/j.bmcl.2009.11.032. Epub 2009 Nov 26.
PMID:20005096
Abstract
The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure-activity relationships, attenuation of dopaminergic activity, and potentiation of mGluR2 responses in rat hippocampal MPP-DG synapses are also reported.
摘要
描述了高通量筛选命中系列（1）的优化，从而鉴定出结构新颖、选择性、可口服生物利用的 mGluR2 正变构调节剂 GSK1331258 和 GSK1331268。还报告了结构活性关系、多巴胺能活性的衰减以及大鼠海马 MPP-DG 突触中 mGluR2 反应的增强。
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