Functional evidence of atypical beta 3-adrenoceptors in the human colon using the beta 3-selective adrenoceptor antagonist, SR 59230A

The role of beta 3-adrenoceptors in human colonic circular smooth muscle was assessed in vitro by use of the beta 3-selective antagonist SR 59230A. Isoprenaline, in the presence of the selective beta-adrenoceptor antagonists CGP 20712A (beta 1) and ICI 118551 (beta 2), both at 0.1 microM, concentrat...

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Bibliographic Details
Published in:British journal of pharmacology 1996-04, Vol.117 (7), p.1374-1376
Main Authors: De Ponti, F, Gibelli, G, Croci, T, Arcidiaco, M, Crema, F, Manara, L
Format: Article
Language:English
Subjects:
Adrenergic beta-Agonists - pharmacology
Adrenergic beta-Antagonists - pharmacology
Aged
Colon
Female
Humans
In Vitro Techniques
Isoproterenol - pharmacology
Male
Middle Aged
Muscle Relaxation - drug effects
Muscle, Smooth - drug effects
Muscle, Smooth - metabolism
Propanolamines - pharmacology
Receptors, Adrenergic, beta - metabolism
Receptors, Adrenergic, beta-3
Stereoisomerism
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Summary:The role of beta 3-adrenoceptors in human colonic circular smooth muscle was assessed in vitro by use of the beta 3-selective antagonist SR 59230A. Isoprenaline, in the presence of the selective beta-adrenoceptor antagonists CGP 20712A (beta 1) and ICI 118551 (beta 2), both at 0.1 microM, concentration-dependently relaxed the preparation (pEC50 = 5.22). This effect was potently and competitively antagonized by SR 59230A with a pA2 of 8.31, while its R,R enantiomer SR 59483A gave an apparent pKB of 6.21. Relaxation was likewise produced by CGP 12177A (pEC50 = 6.05), but not by BRL 37344. Although only one of these beta 3-selective agonists was effective, the remarkably high potency of SR 59230A as a stereospecific antagonist of non-beta 1 non-beta 2 relaxation of human colonic muscle by isoprenaline provides strong functional evidence of beta 3-adrenoceptors in that tissue.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1996.tb15294.x