Kamei J, Iwamoto Y, Misawa M, Nagase H, Kasuya Y
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
Nihon Shinkei Seishin Yakurigaku Zasshi. 1994 Jun;14(3):147-52.
The effects of streptozotocin-induced diabetes on the antitussive effect of (+/-) pentazocine were examined in mice. Intracerebroventricular (i.c.v.) administration of (+/-) pentazocine produced a dose-dependent antitussive effect in both diabetic and non-diabetic mice. There were no significant differences in the antitussive effect of (+/-) pentazocine in diabetic and non-diabetic mice. The antitussive effect of i.c.v. (+/-) pentazocine was partially, but significantly, reduced in non-diabetic mice following pretreatment with either beta-funaltrexamine, a selective mu-opioid antagonist, or rimcazole, a specific sigma-site antagonist. The antitussive effect of (+/-) pentazocine in diabetic mice was significantly antagonized by pretreatment with rimcazole. However, beta-funaltrexamine had no effect on the antitussive effect of (+/-) pentazocine in diabetic mice. Furthermore, nor-binaltorphimine, a selective kappa-opioid receptor antagonist, had no significant effect on the antitussive effect of (+/-) pentazocine in either non-diabetic or diabetic mice. These results suggest that although the antitussive effect of i.c.v. (+/-) pentazocine in non-diabetic mice is mediated by both mu-opioid receptors and sigma-sites, in diabetic mice this effect is mainly mediated by sigma-sites.
研究了链脲佐菌素诱导的糖尿病对小鼠中（±）喷他佐辛镇咳作用的影响。脑室内（i.c.v.）给予（±）喷他佐辛在糖尿病小鼠和非糖尿病小鼠中均产生剂量依赖性镇咳作用。（±）喷他佐辛在糖尿病小鼠和非糖尿病小鼠中的镇咳作用无显著差异。在非糖尿病小鼠中，用选择性μ阿片受体拮抗剂β-芬太尼或特异性σ位点拮抗剂利姆卡唑预处理后，i.c.v.（±）喷他佐辛的镇咳作用部分但显著降低。利姆卡唑预处理可显著拮抗（±）喷他佐辛在糖尿病小鼠中的镇咳作用。然而，β-芬太尼对（±）喷他佐辛在糖尿病小鼠中的镇咳作用无影响。此外，选择性κ阿片受体拮抗剂去甲丙氧芬对（±）喷他佐辛在非糖尿病或糖尿病小鼠中的镇咳作用均无显著影响。这些结果表明，虽然i.c.v.（±）喷他佐辛在非糖尿病小鼠中的镇咳作用由μ阿片受体和σ位点介导，但在糖尿病小鼠中，这种作用主要由σ位点介导。
