一种选择性δ-阿片受体拮抗剂ICI 174864的中枢效应。

Central effects of a selective delta-opioid receptor antagonist, ICI 174864.

作者信息

Herman Z S, Stańda J, Janas P, Gołba K

出版信息

Pol J Pharmacol Pharm. 1986 Sep-Dec;38(5-6):455-60.

Abstract

Leu-enkephalin (LENK) injected intracerebroventricularly (icv) in a dose of 50-400 micrograms to male Wistar rats inhibited their open field locomotor activity. This effect was antagonized by 1 microgram icv of ICI 174864 but not by naloxone (NAL). Doses of 5 and 10 micrograms of ICI 174864 icv induced a characteristic abnormal behavioral syndrome, which was inhibited by icv LENK, but not by morphine. ICI 174864 potentiated the analgesic effect of morphine, whereas NAL inhibited it. The results indicate that ICI 174864 is an antagonist of central delta-opioid receptors. The abnormal behavior induced by higher doses of ICI 174864 is suggested as an experimental model for studying the central delta-opioid receptors.

摘要

向雄性Wistar大鼠脑室内注射剂量为50 - 400微克的亮氨酸脑啡肽（LENK）会抑制其旷场运动活动。这种作用可被脑室内注射1微克的ICI 174864拮抗，但不能被纳洛酮（NAL）拮抗。脑室内注射5微克和10微克的ICI 174864会诱发一种特征性的异常行为综合征，该综合征可被脑室内注射的LENK抑制，但不能被吗啡抑制。ICI 174864增强了吗啡的镇痛作用，而NAL则抑制了它。结果表明，ICI 174864是中枢δ阿片受体的拮抗剂。较高剂量的ICI 174864诱发的异常行为被建议作为研究中枢δ阿片受体的实验模型。