mGluR5 变构调节剂的功效切换 SAR：一种化学结构类型的高活性正调节剂和负调节剂。
Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.
机构信息
Discovery Chemistry and DMPK, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark.
出版信息
Bioorg Med Chem Lett. 2011 Jun 1;21(11):3407-10. doi: 10.1016/j.bmcl.2011.03.103. Epub 2011 Apr 5.
PMID:21531137
Abstract
A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the underlying SAR is detailed.
摘要
本文描述了一系列代谢型谷氨酸 5 型受体（mGluR5）变构配体，它们具有正、负或无调节作用。该系列化合物能够产生具有单数字纳摩尔效力的 mGluR5 PAMs 和 NAMs，这是不寻常的，并且详细描述了潜在的 SAR。
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