Effects of diabetes on the antinociceptive effect of (+/-)pentazocine in mice.

J Kamei, Y Iwamoto, M Misawa, H Nagase, Y Kasuya
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Abstract

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.

糖尿病对小鼠(+/-)戊唑嗪抗伤感受作用的影响。
研究了戊唑嗪(+/-)对链脲佐菌素诱导的糖尿病小鼠的抗伤性作用。虽然(+/-)戊唑嗪(10 nmol)脑室注射对非糖尿病小鼠和糖尿病小鼠均有显著的抗伤害性作用,但(+/-)戊唑嗪在糖尿病小鼠中的抗伤害性作用大于非糖尿病小鼠。(+/-)戊唑嗪对糖尿病和非糖尿病小鼠的抗痛觉作用均被选择性阿片受体拮抗剂-去甲萘多啡胺显著拮抗。另一方面,(+/-)戊唑嗪的抗伤性作用在非糖尿病小鼠中被β -funaltrexamine(一种选择性的mu-阿片受体拮抗剂)预处理后得到增强。此外,(+/-)戊唑嗪在糖尿病小鼠和-富纳曲胺治疗的非糖尿病小鼠之间的抗伤害性作用无显著差异。这些结果表明,mu-阿片受体的低反应性可能解释了(+/-)戊唑嗪在糖尿病小鼠中增强的kappa-阿片受体介导的抗感知作用。
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