NOVEL METABOTROPIC GLUTAMATE-RECEPTOR AGONIST - (2S,1'S,2'R,3'R)-2-(2-CARBOXY-3-METHOXYMETHYLCYCLOPROPYL)GLYCINE (CIS-MCG-I)

被引：31
|
作者：
ISHIDA, M
SAITOH, T
NAKAMURA, Y
KATAOKA, K
SHINOZAKI, H
机构：
[1] TOKYO METROPOLITAN INST MED SCI,DEPT PHARMACOL,BUNKYO KU,TOKYO 113,JAPAN
[2] EHIME UNIV,SCH MED,DEPT PHYSIOL,SHIGENOBU,EHIME 79102,JAPAN
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1994年 / 268卷 / 02期
关键词：
METABOTROPIC GLUTAMATE RECEPTOR; SPINAL CORD; ISOLATED; CAMP; PHOSPHOINOSITIDE HYDROLYSIS; L-CCG-I((2S; I'S; 2'S)-CCG); CORTICAL CELL CULTURE; ACPD ((1S,3R)-1-AMINOCYCLOPENTANE-1,3-DICARBOXYLATE);
D O I：
10.1016/0922-4106(94)90198-8
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A novel agonist for metabotropic glutamate receptors, (2S,1'S,2'R,3'R)-2-(2-carboxy-3-methoxymethylcyclop ropyl)glycine (cis-MCG-I), effectively inhibited monosynaptic excitation in newborn rat spinal cords with EC(50) of 3 mu M 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 mu M. 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.
引用
收藏
页码：267 / 270
页数：4
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