[125I]PIP HOE 140，一种用于缓激肽B2受体的高亲和力放射性配体。

[125I]PIP HOE 140, a high affinity radioligand for bradykinin B2 receptors.

作者信息

Brenner N J, Stonesifer G Y, Schneck K A, Burns H D, Ransom R W

机构信息

Merck Research Laboratories, Department of New Lead Pharmacology, West Point, PA 19486.

出版信息

Life Sci. 1993;53(25):1879-86. doi: 10.1016/0024-3205(93)90027-z.

DOI:10.1016/0024-3205(93)90027-z

PMID:8255148

Abstract

A high affinity radioligand for bradykinin B2 receptors was prepared by coupling an activated ester of [125I]4-iodobenzoic acid to the amino terminus nitrogen of the potent B2 antagonist HOE 140. The ligand, [125I]para-iodophenyl HOE 140 ([125I]PIP HOE 140), bound to a homogeneous set of sites in guinea pig ileal membranes with an equilibrium dissociation constant of 15 pM and a maximal binding density of 193 fmole/mg protein. Competition studies with a number of BK-related peptides indicated that the ligand specifically labeled B2 receptors in the preparation. The results suggest that [125I]PIP HOE 140 will be a useful tool for future studies of B2 receptors.

摘要

通过将[125I]4-碘苯甲酸的活化酯与强效B2拮抗剂HOE 140的氨基末端氮原子偶联，制备了一种用于缓激肽B2受体的高亲和力放射性配体。该配体[125I]对碘苯基HOE 140（[125I]PIP HOE 140）以15 pM的平衡解离常数和193 fmole/mg蛋白质的最大结合密度与豚鼠回肠膜中的一组同质位点结合。用多种与缓激肽相关的肽进行的竞争研究表明，该配体在制剂中特异性标记了B2受体。结果表明，[125I]PIP HOE 140将成为未来研究B2受体的有用工具。