Agonists of cyclic AMP-coupled metabotropic glutamate receptors in adult rat cortical slices

被引：25
作者：
Kemp, MC [1 ]
Jane, DE [1 ]
Tse, HW [1 ]
Roberts, PJ [1 ]
机构：
[1] UNIV BRISTOL,SCH MED SCI,DEPT PHARMACOL,BRISTOL BS8 1TD,AVON,ENGLAND
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1996年 / 309卷 / 01期
基金：
英国医学研究理事会;
关键词：
metabotropic glutamate receptor; cerebral cortex slice; cAMP; (agonist);
D O I：
10.1016/0014-2999(96)00314-7
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A number of potential Group 2 and Group 3 metabotropic glutamate receptor (rr,Glu receptor) agonists were investigated in adult rat brain cerebrocortical slices. The rank order of their potency in inhibiting forskolin-stimulated adenylyl cyclase was found to be: (S)-2-amino-2-methyl-4-phosphonobutyric acid (MAP4) > (2S,1'S,2'S)-2-(2-carboxycyclopropyl)glycine (L-CCG-I) > (1S,3S)-1-aminocyclopentane-1,3-dicarboxylic acid (1S,3S-ACPD) > (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid (1S,3R)-ACPD) > (2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV)> (S)-2-methylglutamate ((S)-MG) > L-glutamate > (2S,1'S,2'S)-2-(2- carboxycyclopropyl)alanine (MCCG)> L-2-amino-4-phosphonobutyric acid (L-AP4) > L-serine-O-phosphate (SOP). The finding that (S)-2-amino-2-methyl-4-phosphonobutyric acid was the most potent agonist at these metabotropic glutamate receptors is in contrast to its observed potent mGlu receptor antagonist action in the neonatal rat spinal cord.
引用
收藏
页码：79 / 85
页数：7
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