肾膜上高亲和力布美他尼受体的特性研究

Characterization of a high affinity piretanide receptor on kidney membranes.

作者信息

Giesen-Crouse E M, Welsch C, Imbs J L, Schmidt M, Schwartz J

出版信息

Eur J Pharmacol. 1985 Aug 7;114(1):23-31. doi: 10.1016/0014-2999(85)90516-3.

Abstract

The tritiated loop diuretic, piretanide, is a useful ligand for specific diuretic receptors which are present in the plasma membranes of renal medullary cells. Its high specific activity (30 Ci X mmol-1) made it possible to demonstrate the existence of a high affinity receptor (Kd approximately 5 nM) and a binding site with low affinity. High affinity binding is saturable, reversible and displaceable by a number of non-radioactive loop diuretics. Structural analogues, devoid of diuretic activity, do not displace piretanide binding. No specific binding occurs in liver or spleen membranes.

摘要

氚标记的袢利尿剂吡咯他尼是一种针对存在于肾髓质细胞质膜中的特定利尿剂受体的有用配体。其高比活度（30 Ci·mmol⁻¹）使得能够证明存在高亲和力受体（解离常数Kd约为5 nM）和低亲和力结合位点。高亲和力结合具有饱和性、可逆性，并且可被多种非放射性袢利尿剂取代。缺乏利尿活性的结构类似物不能取代吡咯他尼的结合。在肝或脾细胞膜中不发生特异性结合。