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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]
- 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