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[Stimulation of adenylate cyclase by the isoforms of human and rat beta-3 adrenergic receptor expressed in the CHO cells]

[Stimulation of adenylate cyclase by the isoforms of human and rat beta-3 adrenergic receptor expressed in the CHO cells]

Authors :
S, Levasseur
C, Pigeon
F, Reyl-Desmars
D, Caput
M J, Lewin
Source :
Gastroenterologie clinique et biologique. 19(8-9)
Publication Year :
1995

Abstract

The beta 3 adrenergic receptor stimulates lipolysis and colonic relaxation in the rat, and, suggestively, in man. Several human forms generated by different mRNA splicings can occur: the A form of 396 amino acids and the B and C forms extended by 12 and 6 amino acids respectively, in the C-terminus region. In order to characterize these different forms as expressed in CHO cells, we studied adenylyl cyclase stimulation by the beta 3 agonists, SR58611A and BRL37344 and its inhibition by the beta 3 antagonist SR59230.This antagonist totally inhibited SR58611-adenylyl cyclase stimulation with the following hierarchy of potency: C formBA. In rat, a unique form is expressed which is close to the human B form. This form was the less sensitive to beta 1 and beta 2 antagonists.These findings constitute a molecular pharmacological basis for the design of beta 3 agonists of therapeutic value.

Details

Language :
French
ISSN :
03998320
Volume :
19
Issue :
8-9
Database :
OpenAIRE
Journal :
Gastroenterologie clinique et biologique
Accession number :
edsair.pmid..........a4918573268551b85b602e09b7a99dd7