Kamei J, Iwamoto Y, Misawa M, Nagase H, Kasuya Y
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
Res Commun Chem Pathol Pharmacol. 1994 Apr;84(1):105-10.
The antinociceptive effect of (+/-)pentazocine was examined in streptozotocin-induced diabetic mice. Although intracerebroventricular (i.c.v.) administration of (+/-)pentazocine (10 nmol) produced a significant antinociceptive effect in both non-diabetic and diabetic mice, the antinociceptive effect of (+/-)pentazocine was greater in diabetic mice than in non-diabetic mice. The antinociceptive effects of (+/-)pentazocine in both diabetic and non-diabetic mice were significantly antagonized by s.c. administration of nor-binaltorphimine, a selective kappa-opioid receptor antagonist. On the other hand, the antinociceptive effects of (+/-)pentazocine were potentiated when non-diabetic mice were pretreated with beta-funaltrexamine, a selective mu-opioid receptor antagonist. Furthermore, there was no significant difference in the antinociceptive effect of (+/-)pentazocine between diabetic mice and beta-funaltrexamine-treated non-diabetic mice. These results suggest that the hypo-responsiveness of mu-opioid receptors may account for the enhanced kappa-opioid receptor-mediated antinociceptive effect of (+/-)pentazocine in diabetic mice.
研究了(±)喷他佐辛在链脲佐菌素诱导的糖尿病小鼠中的抗伤害感受作用。尽管脑室内(i.c.v.)注射(±)喷他佐辛(10 nmol)在非糖尿病和糖尿病小鼠中均产生了显著的抗伤害感受作用,但(±)喷他佐辛在糖尿病小鼠中的抗伤害感受作用比在非糖尿病小鼠中更强。皮下注射选择性κ-阿片受体拮抗剂诺宾那托啡,可显著拮抗(±)喷他佐辛在糖尿病和非糖尿病小鼠中的抗伤害感受作用。另一方面,当用选择性μ-阿片受体拮抗剂β-氟诺啡肽预处理非糖尿病小鼠时,(±)喷他佐辛的抗伤害感受作用增强。此外,糖尿病小鼠与β-氟诺啡肽处理的非糖尿病小鼠之间,(±)喷他佐辛的抗伤害感受作用无显著差异。这些结果表明,μ-阿片受体反应性降低可能是(±)喷他佐辛在糖尿病小鼠中κ-阿片受体介导的抗伤害感受作用增强的原因。