阿片类药物刺激大脑中的低 Km GTP 酶。

Opiates stimulate low Km GTPase in brain.

作者信息

Franklin P H, Hoss W

出版信息

J Neurochem. 1984 Oct;43(4):1132-5. doi: 10.1111/j.1471-4159.1984.tb12853.x.

DOI:10.1111/j.1471-4159.1984.tb12853.x

Abstract

Low Km GTP hydrolysis in rat brain is stimulated in a concentration-dependent manner by the opiate alkaloid etorphine, and by the opioid peptide D-Ala2-leucine-enkephalinamide. The opiate antagonist naloxone inhibits the maximal D-Ala2-leucine-enkephalinamide stimulation of the GTPase, also with concentration dependency. The magnitude of maximally stimulated, opioid-sensitive, GTP hydrolysis is differentially distributed across brain regions. Opioid-stimulated GTPase may represent one means of identifying a specific type of opioid receptor.

摘要

大鼠脑中低 Km 的 GTP 水解可被阿片生物碱埃托啡和阿片肽 D-丙氨酸 2-亮氨酸-脑啡肽酰胺以浓度依赖的方式刺激。阿片拮抗剂纳洛酮也以浓度依赖的方式抑制 D-丙氨酸 2-亮氨酸-脑啡肽酰胺对 GTP 酶的最大刺激作用。最大刺激的、阿片敏感的 GTP 水解幅度在不同脑区有差异分布。阿片刺激的 GTP 酶可能是鉴定特定类型阿片受体的一种方法。