对PHCCC支架的重新探索：发现改进的代谢型谷氨酸受体4正变构调节剂
Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4.
作者信息
Williams Richard, Zhou Ya, Niswender Colleen M, Luo Qingwei, Conn P Jeffrey, Lindsley Craig W, Hopkins Corey R
机构信息
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
出版信息
ACS Chem Neurosci. 2010 Jun 16;1(6):411-419. doi: 10.1021/cn9000318.
Abstract
This Letter describes a detailed SAR analysis of the mGluR4 positive allosteric modulator, PHCCC. We have now developed compounds with improved potency and efficacy; in addition, compounds are presented that show selectivity for mGluR4 versus the other mGluR subtypes.
摘要
本信函描述了对亲代谢型谷氨酸受体4（mGluR4）正向变构调节剂PHCCC的详细构效关系分析。我们现已开发出具有更高效力和功效的化合物；此外，还展示了对mGluR4相对于其他亲代谢型谷氨酸受体亚型具有选择性的化合物。
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