Receptor binding, cGMP stimulation and receptor desensitization by atrial natriuretic peptides in cultured A 10 vascular smooth muscle cells

FEBS Letters

Neuser, Dieter¹  Bellemann, Peter¹ 

[1] ATR-Hypertension, Research Center, Bayer AG, PO Box 10 17 09, D-5600 Wuppertal 1, FRG

关键词: Atrial natriuretic peptide;    Receptor binding;    cyclic GMP;    cyclic AMP;    Receptor desensitization (Vascular smooth muscle. A10 cell;    CRL 1476 cell);   

DOI  :  10.1016/0014-5793(86)81140-1

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Receptor characteristics for atrial natriuretic peptides (ANP) were demonstrated in the permanent tissue culture system of vascular smooth muscle cell (VSMC) line. ¹²⁵I-ANP exhibited reversible and saturable binding to A10 rat VSMC, and the equilibrium dissociation constant, K _d was 157 pM and maximal binding capacity, .B _max amounted to 115 of protein. Binding of the ¹²⁵I-ligand was highly specific for certain potently displacing ANP analogues with inhibition constants (K _i values) in the nano- or even subnanomolar concentration range. Pretreatment of VSMC with ANP yielded receptor desensitization to one half of the ANP receptor density, and supports the conclusion of receptor autoregulation by ANP in A10 VSMC. The receptor coupled intracellular cGMP system was stimulated, and thus demonstrates the application of A10 cells as a model for the study of ANP receptor interaction involved in vascular smooth muscle relaxation.

【 授权许可】

Unknown