[3H]-咪唑克生结合研究揭示人足月子宫肌层环形和纵形肌层中不同的α2-肾上腺素能受体密度。

Different alpha 2-adrenoceptor densities in the circular and longitudinal layers of human near-term myometrium as revealed by [3H]-idazoxan binding studies.

作者信息

Breuiller M, Rouot B, Leroy M J, Blot P, Ferré F

机构信息

INSERM U.166, Maternité Baudelocque, Paris, France.

出版信息

Gynecol Obstet Invest. 1988;26(1):14-20. doi: 10.1159/000293666.

DOI:10.1159/000293666

PMID:2901998

Abstract

[3H]-idazoxan, a specific alpha 2-adrenoceptor antagonist radioligand, has been used to characterize alpha 2-adrenoceptors in both circular and longitudinal layers of human near-term myometrium. [3H]-idazoxan binding is reversible, saturable and stereospecific. It labels with high affinity a single population of sites. Competition curves with different alpha 2-adrenoceptor agonists and antagonists show that the binding sites labelled with [3H]-idazoxan have the pharmacological characteristics of alpha 2-adrenoceptors. Though the KD value is similar in both layers (approximately 7 nM), the density of alpha 2-adrenoceptors in the circular layer (324 +/- 21 fmol/mg of protein) is significantly higher than in the longitudinal one (183 +/- 48 fmol/mg of protein).

摘要

[3H]-咪唑克生是一种特异性α2-肾上腺素能受体拮抗剂放射性配体，已被用于表征人类足月子宫肌层环形和纵形肌层中的α2-肾上腺素能受体。[3H]-咪唑克生结合是可逆的、可饱和的且具有立体特异性。它以高亲和力标记单一的位点群体。不同α2-肾上腺素能受体激动剂和拮抗剂的竞争曲线表明，用[3H]-咪唑克生标记的结合位点具有α2-肾上腺素能受体的药理学特征。尽管两层中的KD值相似（约7 nM），但环形肌层中α2-肾上腺素能受体的密度（324±21 fmol/mg蛋白质）显著高于纵形肌层（183±48 fmol/mg蛋白质）。