A V1-VASCULAR VASOPRESSIN ANTAGONIST SUITABLE FOR RADIOIODINATION AND PHOTOAFFINITY-LABELING

被引：8

作者：

THIBONNIER, M

CHEHADE, N

HINKO, A

机构：

[1] The Division of Hypertension, Department of Medicine, University Hospitals of Cleveland, Case Western Reserve University School of Medicine, Cleveland, OH

[2] Department of Medicine, Medical College of Ohio, Cleveland, OH

来源：

AMERICAN JOURNAL OF HYPERTENSION | 1990年 / 3卷 / 06期

关键词：

Photoaffinity labeling; Radioiodination; Vasopressin;

D O I：

10.1093/ajh/3.6.471

中图分类号：

R6 [外科学];

学科分类号：

1002 ; 100210 ;

摘要：

We have previously characterized the Vl-vascular arginine vasopressin (AVP) receptors of human platelets (Thibonnier M, J Biol Chem 1987;262: 10960-10964). We now report on a radiomonoiodin-ated and photoreactive Vl-vascular AVP antagonist (Vl-ag) to be used for the purification of human Vl-vascular AVP receptors.The Vl-ag, d(CH2)5Tyr(Me)Tyr(NH2)AVP was modified by radiomonoiodination of d(CH2)5-Tyr(Me)Tyr(NH2)AVP with the Iodogen technique, and derivatization of d(CH2)5Tyr(Me)Tyr[125I](NH2)-AVP with the photoreactive crosslinker, N-hydrox-ysuccinimidyl-4-azidobenzoate (HSAB) (each step included HPLC purification).In competition experiments, the affinity of these Vl-ag for the human platelet AVP receptors remained excellent:Compound Ki(nmol/L) d(CH2)5Tyr(Me)AVP 1.50 ±0.20 d(CH2)5Tyr(Me)Tyr(NH2)AVP 5.26 ±0.41 d(CH2)5Tyr(Me)Tyr[125I](NH2)AVP 2.76 ± 0.23 AzBz-d(CH2)5Tyr(ME)Tyr[125I](NH2)AVP 2.32 ± 0.32 Irreversible photoaffinity labeling of the platelet Vl-vascular AVP receptor was successfully achieved by UV lamp exposure (365 nm, 20 min). Thus, AzBz-d(CH2)5Tyr(Me)Tyr[125I](NH2)AVP is a promising tool to use for the purification of human Vl-vascular AVP receptors. © 1990 by the American Journal of Hypertension, Ltd.

引用

页码：471 / 475

页数：5

共 17 条

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