Govek Steven P, Bonnefous Celine, Hutchinson John H, Kamenecka Theodore, McQuiston Jeffrey, Pracitto Richard, Zhao Lucy X, Gardner Michael F, James Joyce K, Daggett Lorrie P, Rowe Blake A, Schaffhauser Hervé, Bristow Linda J, Campbell Una C, Rodriguez Dana E, Vernier Jean-Michel
Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2005 Sep 15;15(18):4068-72. doi: 10.1016/j.bmcl.2005.06.017.
Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.
代谢型谷氨酸受体2（mGluR2）已被认为与包括精神分裂症在内的多种中枢神经系统疾病有关。本文公开了一系列新型mGluR2变构增强剂的研发情况。结合药代动力学数据进行的构效关系研究导致了吲哚5的发现，其在精神分裂症动物模型中具有活性。
