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苯环利定与(-)喷他佐辛(而非(+)喷他佐辛)之间的交叉致敏作用。

Cross-sensitization between phencyclidine and (-) but not (+) pentazocine.

作者信息

Xu X, Domino E F

机构信息

Department of Pharmacology, University of Michigan, Ann Arbor 48109-0632, USA.

出版信息

Pharmacol Biochem Behav. 1997 Feb;56(2):205-10. doi: 10.1016/s0091-3057(96)00215-8.

Abstract

Repeated administration of psychomotor stimulants such as amphetamine and cocaine, and psychotomimetics such as phencyclidine, produce progressively enhanced behavioral effects, a phenomenon known as behavioral sensitization. Little is known about the effects of repeated treatment with sigma ligands on locomotor activity. The present research determined the psychomotor stimulant effects of the sigma ligand (+)pentazocine and its enantiomer; and investigated whether reciprocal cross-sensitization occurs between them and PCP-induced locomotor activity and ambulation. Adult female Sprague-Dawley rats were used. Total locomotor activity and ambulation were assessed with an automated photoelectric system. Acute (+) or (-)pentazocine given IP produced slight but insignificant locomotor stimulant effects. Repeated administration of (+)pentazocine failed to produce behavioral sensitization. However, four repeated injections of (-)pentazocine or PCP produced behavioral sensitization. (-)Pentazocine sensitized rats showed cross-sensitization to PCP-induced locomotion and ambulation. Furthermore, PCP sensitized rats showed cross-sensitization to (-)pentazocine-induced locomotion and ambulation. These findings suggest that (+) and (-)pentazocine act at different receptor sites. (-)Pentazocine is more similar to PCP in producing locomotor stimulant effects.

摘要

重复给予苯丙胺和可卡因等精神运动性兴奋剂以及苯环利定等拟精神病药物,会产生逐渐增强的行为效应,这一现象被称为行为敏化。关于重复使用西格玛配体对运动活动的影响,人们了解甚少。本研究确定了西格玛配体(+)喷他佐辛及其对映体的精神运动性兴奋作用;并研究了它们与苯环利定诱导的运动活动和行走之间是否发生相互交叉敏化。使用成年雌性斯普拉格-道利大鼠。用自动光电系统评估总运动活动和行走情况。腹腔注射急性给予(+)或(-)喷他佐辛产生轻微但不显著的运动兴奋作用。重复给予(+)喷他佐辛未能产生行为敏化。然而,四次重复注射(-)喷他佐辛或苯环利定产生了行为敏化。(-)喷他佐辛致敏的大鼠对苯环利定诱导的运动和行走表现出交叉敏化。此外,苯环利定致敏的大鼠对(-)喷他佐辛诱导的运动和行走表现出交叉敏化。这些发现表明(+)和(-)喷他佐辛作用于不同的受体位点。(-)喷他佐辛在产生运动兴奋作用方面与苯环利定更为相似。

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