Selective receptors for β-endorphin on the rat vas deferens
Selective receptors for β-endorphin on the rat vas deferens
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DOI：
10.1016/0024-3205(79)90368-0
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发表时间：
1979-02
期刊：
影响因子：
6.1
通讯作者：
R. Schulz;E. Faase;M. Wüster;A. Herz
中科院分区：
文献类型：
--
作者：
R. Schulz;E. Faase;M. Wüster;A. Herz
离体大鼠输精管对吗啡不敏感，含有β-内啡肽的选择性结合位点。用100 nM β-内啡肽建立了对电刺激诱发的抽搐张力的半数最大抑制，而β-内啡肽片段，即甲硫氨酸-脑啡肽、α-内啡肽和γ-内啡肽几乎无效。阿片类生物碱埃托啡是豚鼠回肠和小鼠输精管的强效抑制剂，但对大鼠输精管的作用要小100倍。独特的β-内啡肽活性表明该肽具有非常特异的结合位点，这与迄今为止在分离制剂上描述的阿片类药物的μ-或δ-受体无关。
The isolated rat vas deferens, being insensitive to morphine, contains selective binding sites for β-end-orphin. A half-maximal inhibition of twitch tension evoked by electrical stimulation is established with 100 nM β-endorphin, while fragments of β-endorphin, that is, methionine-enkephalin, α- and γ-endorphin, are almost ineffective. The opiate alkaloid etorphine, a powerful inhibitor of guinea-pig ileum and mouse vas deferens, is 100-fold less potent on the rat vas deferens. The unique β-endorphin activity suggests very specific binding sites for this peptide, which cannot be related to the μ- or δ-receptors so far described for opiods on isolated preparations.