Glutamate release inhibiting properties of the novel mGlu5 receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP):: complementary in vitro and in vivo evidence

被引:44
作者
Thomas, LS
Jane, DE
Gasparini, F
Croucher, MJ
机构
[1] Charing Cross Hosp, Sch Med, Imperial Coll, Dept Neuroinflammat, London W6 8RF, England
[2] Sch Med Sci Bristol, Dept Pharmacol, Bristol BS8 1TD, Avon, England
[3] Novartis Pharma AG, Therapeut Area Nervous Syst, CH-4002 Basel, Switzerland
基金
英国惠康基金;
关键词
glutamate; metabotropic glutamate receptors; autoreceptors; presynaptic; MPEP;
D O I
10.1016/S0028-3908(01)00091-0
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
We have previously demonstrated that neuronal release of the excitatory amino acid glutamate is facilitated by the selective activation of presynaptic Group I metabotropic autoreceptors. Here we report the release inhibiting actions of the novel mGlu(5) receptor-selective antagonist, 2-methyl-6-(phenylethynyl)-pyridine (MPEP), both in vitro and in vivo. These data provide compelling evidence for the presence of functional positive modulatory mGlu(5) subtype autoreceptors in the mammalian central nervous system. (C) 2001 Published by Elsevier Science Ltd.
引用
收藏
页码:523 / 527
页数:5
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