Stereospecific binding of propranolol and catecholamines to the beta-adrenergic receptor.

Abstract:

:The stereospecificity of the beta-adrenergic receptor of turkey erythrocyte ghosts was studied. Binding of the specific beta-adrenergic antagonist, propranolol, was found to occur exclusively with the l-stereoisomer. The stereospecificity of catecholamine binding was determined by assaying the ability of the catecholamines to displace [(3)H]propranolol. Binding of the catecholamines was also found to be stereospecific for the l-stereoisomers. Furthermore, the d-stereoisomers do not compete with the l form for binding. Using this displacement technique, we were able to calculate the dissociation constants for l-epinephrine, l-norepinephrine, and l-isoproterenol from the beta-receptor and compare these values to the apparent dissociation constants obtained from the direct activation of adenylate cyclase (EC 4.6.1.1) by these catecholamines.

authors

Atlas D,Steer ML,Levitzki A

doi

10.1073/pnas.71.10.4246

subject

Has Abstract

pub_date

1974-10-01 00:00:00

pages

4246-8

issue

10

eissn

0027-8424

issn

1091-6490

journal_volume

71

pub_type

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