阿片κ激动剂对大鼠红细胞血影钙泵的可能抑制作用。

Possible inhibition of Ca++ pump of rat erythrocyte ghosts by opioid k agonists.

作者信息

Yamasaki Y, Way E L

出版信息

Life Sci. 1983;33 Suppl 1:723-6. doi: 10.1016/0024-3205(83)90604-5.

PMID:6319922

Abstract

Rat erythrocyte ghosts containing 45Ca++, EGTA, ATP and Pipes buffer (pH 7.2) were prepared for studying opioid effects on Ca++ flux. Ethylketocyclazocine and dynorphin 1-13 (dynorphin) dose-dependently inhibited La+++-sensitive outward 45Ca++ movement at nM concentrations and the effect was naloxone reversible. Morphine and beta-endorphin were also effective at higher concentrations, whereas levorphanol and leu-enkephalin were ineffective. None of the opioids studied inhibited 45Ca++ inward movement. Based on these findings, it is concluded that rat erythrocyte possesses k-type opioid receptors through which the Ca++-pump may be inhibited.

摘要

制备含有45Ca++、乙二醇双四乙酸（EGTA）、三磷酸腺苷（ATP）和哌嗪-N,N'-双（2-乙磺酸）缓冲液（pH 7.2）的大鼠红细胞血影，用于研究阿片类药物对Ca++通量的影响。乙基酮环唑辛和强啡肽1-13（强啡肽）在纳摩尔浓度下剂量依赖性地抑制镧离子（La+++）敏感的外向45Ca++移动，且该效应可被纳洛酮逆转。吗啡和β-内啡肽在较高浓度时也有效，而左啡诺和亮氨酸脑啡肽则无效。所研究的阿片类药物均未抑制45Ca++内向移动。基于这些发现，得出结论：大鼠红细胞具有k型阿片受体，通过该受体可能抑制Ca++泵。