Matsuno K, Senda T, Kobayashi T, Mita S
Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Osaka, Japan.
Brain Res. 1995 Sep 4;690(2):200-6. doi: 10.1016/0006-8993(95)00618-z.
The effects of the stereoisomers of N-allylnormetazocine (SKF-10,047) on the hippocampal cholinergic functions were compared in rats. A putative sigma 1 receptor agonist, (+)-SKF-10,047, elicited an increase of hippocampal extracellular acetylcholine level and anti-amnesic effect against scopolamine-induced memory dysfunctions in rats. These phenomena were not produced by (-)-SKF-10,047, and were reversed by haloperidol, a putative sigma 1 receptor antagonist. Such stereoselectivity and antagonism imply an involvement of sigma 1 receptors in these (+)-SKF-10,047-stimulated hippocampal cholinergic functions.
在大鼠中比较了N-烯丙基去甲左啡诺(SKF-10,047)的立体异构体对海马胆碱能功能的影响。一种假定的σ1受体激动剂,(+)-SKF-10,047,可引起大鼠海马细胞外乙酰胆碱水平升高,并对东莨菪碱诱导的记忆功能障碍具有抗遗忘作用。这些现象不是由(-)-SKF-10,047产生的,并且被一种假定的σ1受体拮抗剂氟哌啶醇所逆转。这种立体选择性和拮抗作用表明σ1受体参与了这些(+)-SKF-10,047刺激的海马胆碱能功能。