促性腺激素释放激素（LHRH）与醋酸那法瑞林（一种高效的LHRH激动剂）的血浆结合情况。

Plasma binding of LHRH and nafarelin acetate, a highly potent LHRH agonist.

作者信息

Chan R L, Chaplin M D

出版信息

Biochem Biophys Res Commun. 1985 Mar 15;127(2):673-9. doi: 10.1016/s0006-291x(85)80214-x.

Abstract

The binding of LHRH and [6-(3-(2-naphthyl)-D-Ala]LHRH (nafarelin acetate), a highly potent LHRH agonist, to plasma proteins was investigated in vitro by equilibrium dialysis at 4 degrees C with fresh plasma from normal human subjects, female rhesus monkeys, and female rats. Over a wide range of concentrations (10(-8) to 10(-5) M), 78-84% of nafarelin acetate and only 22-25% of LHRH were bound to undiluted plasma. With 10% plasma, the extent of binding was 31-37%, and 0.9-4.2% for nafarelin acetate and LHRH, respectively. Albumin was shown to play a predominant role in the plasma binding of the two compounds. The considerable differences in the extent of binding of nafarelin acetate and LHRH to plasma may contribute to some of the differences in pharmacokinetic parameters observed for the two compounds.

摘要

在4℃下，采用平衡透析法，使用来自正常人类受试者、雌性恒河猴和雌性大鼠的新鲜血浆，在体外研究了促性腺激素释放激素（LHRH）和一种高效的LHRH激动剂[6-(3-(2-萘基)-D-丙氨酸]LHRH（醋酸萘法瑞林）与血浆蛋白的结合情况。在很宽的浓度范围（10⁻⁸至10⁻⁵M）内，醋酸萘法瑞林的78 - 84%以及LHRH的仅22 - 25%与未稀释血浆结合。对于10%的血浆，醋酸萘法瑞林和LHRH的结合程度分别为31 - 37%和0.9 - 4.2%。已表明白蛋白在这两种化合物的血浆结合中起主要作用。醋酸萘法瑞林和LHRH与血浆结合程度的显著差异可能是这两种化合物观察到的药代动力学参数差异的部分原因。