一种新型代谢型谷氨酸受体激动剂：(2S,1'S,2'R,3'R)-2-(2-羧基-3-甲氧基甲基环丙基)甘氨酸（顺式-MCG-I）。

A novel metabotropic glutamate receptor agonist: (2S,1'S,2'R,3'R)-2-(2-carboxy-3-methoxymethylcyclopropyl)glycine (cis-MCG-I).

作者信息

Ishida M, Saitoh T, Nakamura Y, Kataoka K, Shinozaki H

机构信息

Department of Pharmacology, Tokyo Metropolitan Institute of Medical Science, Japan.

出版信息

Eur J Pharmacol. 1994 Jul 15;268(2):267-70. doi: 10.1016/0922-4106(94)90198-8.

DOI:10.1016/0922-4106(94)90198-8

PMID:7957649

Abstract

A novel agonist for metabotropic glutamate receptors, (2S,1'S,2'R,3'R)-2-(2-carboxy-3-methoxymethylcyclopropyl)glycine (cis-MCG-I), effectively inhibited monosynaptic excitation in newborn rat spinal cords with EC50 of 3 microM without causing any depolarization. Furthermore, cis-MCG-I inhibited the forskolin-stimulated cyclic AMP formation in rat cultured cortical cells with IC50 of 1.5 microM. cis-MCG-I neither stimulated the phosphoinositide hydrolysis nor activated ionotropic glutamate receptors even in high concentrations. However, after a brief exposure of spinal cords to quisqualate, it caused depolarization in a dose-dependent manner. This compound would provide useful information for elucidating physiological functions of metabotropic glutamate receptors.

摘要

一种新型的代谢型谷氨酸受体激动剂，(2S,1'S,2'R,3'R)-2-(2-羧基-3-甲氧基甲基环丙基)甘氨酸（顺式-MCG-I），能有效抑制新生大鼠脊髓中的单突触兴奋，其半数有效浓度（EC50）为3微摩尔，且不会引起任何去极化。此外，顺式-MCG-I抑制大鼠培养皮层细胞中福斯高林刺激的环磷酸腺苷（cAMP）生成，其半数抑制浓度（IC50）为1.5微摩尔。即使在高浓度下，顺式-MCG-I既不刺激磷酸肌醇水解，也不激活离子型谷氨酸受体。然而，在脊髓短暂暴露于喹啉酸后，它会以剂量依赖的方式引起去极化。该化合物将为阐明代谢型谷氨酸受体的生理功能提供有用信息。