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 29 条
  • [1] Characterization of [3H]-(2S,2′R,3′R)-2-(2′,3′-dicarboxycyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes
    Cartmell, J
    Adam, G
    Chaboz, S
    Henningsen, R
    Kemp, JA
    Klingelschmidt, A
    Metzler, V
    Monsma, F
    Schaffhauser, H
    Wichmann, J
    Mutel, V
    BRITISH JOURNAL OF PHARMACOLOGY, 1998, 123 (03) : 497 - 504
  • [2] POTENTIATION OF EXCITATORY POSTSYNAPTIC POTENTIALS BY A METABOTROPIC GLUTAMATE-RECEPTOR AGONIST (1S,3R-ACPD) IN FROG SPINAL MOTONEURONS
    GOTANI, H
    KUNO, M
    NAKAMURA, F
    MATSUURA, S
    BRAIN RESEARCH, 1995, 689 (02) : 281 - 288
  • [3] (1S,3R)-ACPD, a metabotropic glutamate receptor agonist, enhances damage after global ischaemia
    Henrich-Noack, P
    Reymann, KG
    EUROPEAN JOURNAL OF PHARMACOLOGY, 1999, 365 (01) : 55 - 58
  • [4] MODULATORY EFFECTS OF NMDA ON PHOSPHOINOSITIDE RESPONSES EVOKED BY THE METABOTROPIC GLUTAMATE-RECEPTOR AGONIST 1S,3R-ACPD IN NEONATAL RAT CEREBRAL-CORTEX
    CHALLISS, RAJ
    MISTRY, R
    GRAY, DW
    NAHORSKI, SR
    BRITISH JOURNAL OF PHARMACOLOGY, 1994, 112 (01) : 231 - 239
  • [5] Design, Synthesis, Pharmacology, and In Silico Studies of (1S,2S,3S)-2-((S)-Amino(carboxy)methyl)-3-(carboxymethyl)cyclopropane-1-carboxylic Acid (LBG30300): A Picomolar Potency Subtype-Selective mGlu2 Receptor Agonist
    Liu, Na
    Eshak, Floriane
    Malhaire, Fanny
    Brabet, Isabelle
    Prezeau, Laurent
    Renard, Emma
    Pin, Jean-Philippe
    Acher, Francine C.
    Staudt, Markus
    Bunch, Lennart
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (02) : 1314 - 1326
  • [6] AGONIST ANALYSIS OF 2-(CARBOXYCYCLOPROPYL)GLYCINE ISOMERS FOR CLONED METABOTROPIC GLUTAMATE RECEPTOR SUBTYPES EXPRESSED IN CHINESE-HAMSTER OVARY CELLS
    HAYASHI, Y
    TANABE, Y
    ARAMORI, I
    MASU, M
    SHIMAMOTO, K
    OHFUNE, Y
    NAKANISHI, S
    BRITISH JOURNAL OF PHARMACOLOGY, 1992, 107 (02) : 539 - 543
  • [7] Differential effects of learning and recall of a spatial task on phosphoinositide hydrolysis induced by the metabotropic glutamate receptor agonist 1(S),3(R)-ACPD (1(S),3(R)-1-amino-cyclopentane-1,3-dicarboxylic acid) in the hippocampus and the prefrontal cortex of rats
    deBruin, JPC
    Facchinetti, F
    Toth, E
    Balazs, R
    Joosten, RNJMA
    NEUROSCIENCE LETTERS, 1996, 204 (1-2) : 57 - 60
  • [8] 1S,3R-ACPD-SENSITIVE (METABOTROPIC) [H-3] GLUTAMATE RECEPTOR-BINDING IN MEMBRANES
    SCHOEPP, DD
    TRUE, RA
    NEUROSCIENCE LETTERS, 1992, 145 (01) : 100 - 104
  • [9] INTRACEREBRAL 1S,3R-1-AMINOCYCLOPENTANE-1,3-DICARBOXYLIC ACID (1S,3R-ACPD) PRODUCES LIMBIC SEIZURES THAT ARE NOT BLOCKED BY IONOTROPIC GLUTAMATE-RECEPTOR ANTAGONISTS
    TIZZANO, JP
    GRIFFEY, KI
    JOHNSON, JA
    FIX, AS
    HELTON, DR
    SCHOEPP, DD
    NEUROSCIENCE LETTERS, 1993, 162 (1-2) : 12 - 16
  • [10] 4-BROMOHOMOIBOTENIC ACID SELECTIVELY ACTIVATES A 1-AMINOCYCLOPENTANE-1S,3R-DICARBOXYLIC ACID-INSENSITIVE METABOTROPIC GLUTAMATE-RECEPTOR COUPLED TO PHOSPHOINOSITIDE HYDROLYSIS IN RAT CORTICAL SLICES
    CHUNG, DS
    WINDER, DG
    CONN, PJ
    JOURNAL OF NEUROCHEMISTRY, 1994, 63 (01) : 133 - 139
123