两种全身活性脑啡肽类似物对大鼠抗惊厥作用的比较。

A comparison of the anticonvulsant effects of two systemically active enkephalin analogues in rats.

作者信息

Cowan A, Tortella F C, Adler M W

出版信息

Eur J Pharmacol. 1981 Apr 24;71(1):117-21. doi: 10.1016/0014-2999(81)90392-7.

Abstract

FK-33,824 (Tyr-D-Ala-Gly-MePhe-Met(O)-ol) and metkephamid (Tyr-D-Ala-Gly-Phe-N(Me)Met-CONH2; LY 127623) are two parenterally active synthetic analogues of the endogenous morphinomimetic pentapeptide, [Met5]-enkephalin. Acute s.c. administration of each analogue raised the seizure threshold in a dose-related manner in rats challenged with flurothyl, a volatile convulsant. The anticonvulsant action was antagonized by a low dose of naloxone (0.10 mg/kg s.c.). FK-33,824 and metkephamid can therefore be classified with typical mu-receptor agonists such as morphine and etorphine in this procedure.

摘要

FK - 33824（酪氨酰 - D - 丙氨酰 - 甘氨酰 - 甲基苯丙氨酰 - 甲硫氨酸（氧）醇）和甲硫啡肽（酪氨酰 - D - 丙氨酰 - 甘氨酰 - 苯丙氨酰 - N - 甲基甲硫氨酸 - 羧酰胺；LY 127623）是内源性拟吗啡五肽[甲硫氨酸5] - 脑啡肽的两种肠道外活性合成类似物。对用挥发性惊厥剂氟烷攻击的大鼠进行急性皮下注射每种类似物，均以剂量相关方式提高了惊厥阈值。低剂量纳洛酮（0.10毫克/千克皮下注射）可拮抗这种抗惊厥作用。因此，在此实验过程中，FK - 33824和甲硫啡肽可与典型的μ受体激动剂如吗啡和埃托啡归为一类。