代谢型谷氨酸受体2（mGlu2）的变构增强剂。第3部分：含茚满酮的mGlu2受体增强剂的鉴定及生物学活性
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.
作者信息
Pinkerton Anthony B, Cube Rowena V, Hutchinson John H, James Joyce K, Gardner Michael F, Rowe Blake A, Schaffhauser Hervé, Rodriguez Dana E, Campbell Una C, Daggett Lorrie P, Vernier Jean-Michel
机构信息
Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1565-71. doi: 10.1016/j.bmcl.2005.01.077.
We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50=186 nM), which displayed activity in a rodent model for schizophrenia.
我们已经鉴定并合成了一系列苯基四唑基和4-硫代吡啶基茚满酮，作为代谢型谷氨酸受体2的变构增强剂。旨在提高效力、增强水平以及药代动力学性质的构效关系研究，促成了化合物28（EC50 = 186 nM）的发现，该化合物在啮齿动物精神分裂症模型中显示出活性。
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