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

相关论文

共 15 条

[1] LITHIUM AMPLIFIES AGONIST-DEPENDENT PHOSPHATIDYLINOSITOL RESPONSES IN BRAIN AND SALIVARY-GLANDS [J].

BERRIDGE, MJ ;

DOWNES, CP ;

HANLEY, MR .

BIOCHEMICAL JOURNAL, 1982, 206 (03) :587-595

[2] CHARACTERIZATION OF METABOTROPIC GLUTAMATE RECEPTORS NEGATIVELY LINKED TO ADENYLYL-CYCLASE IN BRAIN-SLICES [J].

GENAZZANI, AA ;

CASABONA, G ;

LEPISCOPO, MR ;

CONDORELLI, DF ;

DELLALBANI, P ;

SHINOZAKI, H ;

NICOLETTI, F .

BRAIN RESEARCH, 1993, 622 (1-2) :132-138

[3] AGONIST ANALYSIS OF 2-(CARBOXYCYCLOPROPYL)GLYCINE ISOMERS FOR CLONED METABOTROPIC GLUTAMATE RECEPTOR SUBTYPES EXPRESSED IN CHINESE-HAMSTER OVARY CELLS [J].

HAYASHI, Y ;

TANABE, Y ;

ARAMORI, I ;

MASU, M ;

SHIMAMOTO, K ;

OHFUNE, Y ;

NAKANISHI, S .

BRITISH JOURNAL OF PHARMACOLOGY, 1992, 107 (02) :539-543

[4] ROLE OF A METABOTROPIC GLUTAMATE-RECEPTOR IN SYNAPTIC MODULATION IN THE ACCESSORY OLFACTORY-BULB [J].

HAYASHI, Y ;

MOMIYAMA, A ;

TAKAHASHI, T ;

OHISHI, H ;

OGAWAMEGURO, R ;

SHIGEMOTO, R ;

MIZUNO, N ;

NAKANISHI, S .

NATURE, 1993, 366 (6456) :687-690

[5] A POTENT METABOTROPIC GLUTAMATE RECEPTOR AGONIST - ELECTROPHYSIOLOGICAL ACTIONS OF A CONFORMATIONALLY RESTRICTED GLUTAMATE ANALOG IN THE RAT SPINAL-CORD AND XENOPUS OOCYTES [J].

ISHIDA, M ;

AKAGI, H ;

SHIMAMOTO, K ;

OHFUNE, Y ;

SHINOZAKI, H .

BRAIN RESEARCH, 1990, 537 (1-2) :311-314

[6] A NOVEL METABOTROPIC GLUTAMATE-RECEPTOR AGONIST - MARKED DEPRESSION OF MONOSYNAPTIC EXCITATION IN THE NEWBORN RAT ISOLATED SPINAL-CORD [J].

ISHIDA, M ;

SAITOH, T ;

SHIMAMOTO, K ;

OHFUNE, Y ;

SHINOZAKI, H .

BRITISH JOURNAL OF PHARMACOLOGY, 1993, 109 (04) :1169-1177

[7] A NEW METABOTROPIC GLUTAMATE-RECEPTOR AGONIST - DEVELOPMENTAL-CHANGE OF ITS SENSITIVITY TO RECEPTORS IN THE NEWBORN RAT SPINAL-CORD [J].

ISHIDA, M ;

SAITOH, T ;

SHINOZAKI, H .

NEUROSCIENCE LETTERS, 1993, 160 (02) :156-158

[8]

NAKAGAWA Y, 1990, EUR J PHARMACOL, V184, P205

[9] (2(S),1'(R),2'(R),3'(R))-2-(2,3-DICARBOXYCYCLOPROPYL)GLYCINE ENHANCES QUISQUALATE-STIMULATED INOSITOL PHOSPHOLIPID HYDROLYSIS IN HIPPOCAMPAL SLICES [J].

NICOLETTI, F ;

CASABONA, G ;

GENAZZANI, AA ;

LEPISCOPO, MR ;

SHINOZAKI, H .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1993, 245 (03) :297-298

[10] RELEASE OF EXCITATORY AMINO-ACIDS FROM CULTURED HIPPOCAMPAL ASTROCYTES INDUCED BY A HYPOXIC-HYPOGLYCEMIC STIMULATION [J].

OGATA, T ;

NAKAMURA, Y ;

SHIBATA, T ;

KATAOKA, K .

JOURNAL OF NEUROCHEMISTRY, 1992, 58 (05) :1957-1959