Butelman E R, Negus S S, Gatch M B, Chang K J, Woods J H
Department of Pharmacology, University of Michigan, Ann Arbor 48109-0632, USA.
Eur J Pharmacol. 1995 Apr 24;277(2-3):285-7. doi: 10.1016/0014-2999(95)00134-7.
The synthetic delta-opioid receptor agonist BW373U86 (0.18-0.56 mg/kg s.c.) was studied in rhesus monkeys with a warm-water, tail-withdrawal assay, designed to detect bradykinin (0.1 microgram) and prostaglandin E2 (5-15.8 micrograms)-induced thermal allodynia. BW373U86 dose-dependently reversed bradykinin allodynia, but was ineffective against prostaglandin E2 allodynia. The BW373U86 dose-effect curve was shifted to the right by the delta-opioid receptor-selective antagonist naltrindole (1.0 mg/kg) but not by the mu-opioid receptor-selective antagonist quadazocine (0.1 mg/kg). The present findings add to the conditions in which delta-opioid receptor-mediated behavioral effects have been detected in primates, and suggest that delta-opioid agonists may be of therapeutic interest in the treatment of some types of hyperalgesic conditions.
采用温水甩尾试验,在恒河猴中研究了合成的δ-阿片受体激动剂BW373U86(皮下注射剂量为0.18 - 0.56毫克/千克),该试验旨在检测缓激肽(0.1微克)和前列腺素E2(5 - 15.8微克)诱导的热痛觉过敏。BW373U86剂量依赖性地逆转缓激肽诱导的痛觉过敏,但对前列腺素E2诱导的痛觉过敏无效。δ-阿片受体选择性拮抗剂纳曲吲哚(1.0毫克/千克)使BW373U86的剂量效应曲线右移,而μ-阿片受体选择性拮抗剂夸达佐辛(0.1毫克/千克)则无此作用。目前的研究结果增加了在灵长类动物中检测到δ-阿片受体介导的行为效应的条件,并表明δ-阿片受体激动剂在治疗某些类型的痛觉过敏情况中可能具有治疗意义。