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σ受体在小鼠运动条件性抑制中所起的作用。

A role played by sigma receptors in the conditioned suppression of motility in mice.

作者信息

Nabeshima T, Kamei H, Kameyama T

机构信息

Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Meijo University, Nagoya, Japan.

出版信息

Psychopharmacology (Berl). 1988;94(4):515-20. doi: 10.1007/BF00212847.

Abstract

Mice exhibited marked suppression of motility (conditioned suppression) when placed in the same environment in which they had previously received an electric footshock. The conditioned suppression was attenuated by cyclazocine and N-allylnormetazocine (SKF-10047), sigma agonists. The effect of these drugs was reduced by chronic pretreatment with cyclazocine. This behavioral change was related to the change in binding activity of [3H]-phencyclidine to sigma receptors (defined using non-radioactive SKF-10047). In the chronic vehicle-pretreated conditioned suppression group, the Kd and Bmax values of [3H]-phencyclidine binding at the high affinity site were increased when compared to those in the chronic vehicle-pretreated control group. The increased values were restored to the control levels by acute treatment with cyclazocine and SKF-10047. On the other hand, in the chronic cyclazocine-pretreated conditioned suppression group, acute cyclazocine and SKF-10047 treatment failed to change the increased values of Kd and Bmax at the high affinity site. The present behavioral and receptor-binding experiments suggest that the activation of nervous system mediated by sigma receptors may be responsible for the attenuation of conditioned suppression of motility.

摘要

当小鼠被置于它们先前曾接受过足部电击的相同环境中时,会表现出明显的运动抑制(条件性抑制)。环唑辛和N-烯丙基去甲左啡诺(SKF-10047)这两种西格玛受体激动剂可减轻这种条件性抑制。这些药物的作用会因环唑辛的慢性预处理而减弱。这种行为变化与[3H]-苯环利定与西格玛受体的结合活性变化有关(使用非放射性SKF-10047进行定义)。在慢性给予赋形剂预处理的条件性抑制组中,与慢性给予赋形剂预处理的对照组相比,[3H]-苯环利定在高亲和力位点的结合Kd值和Bmax值有所增加。通过环唑辛和SKF-10047的急性处理,增加的值恢复到了对照水平。另一方面,在慢性环唑辛预处理的条件性抑制组中,急性给予环唑辛和SKF-10047处理未能改变高亲和力位点Kd值和Bmax值的增加情况。目前的行为和受体结合实验表明,由西格玛受体介导的神经系统激活可能是运动条件性抑制减弱的原因。

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