Characterization of a beta 3-adrenoceptor stimulating gastrin and somatostatin secretions in rat antrum
| Autor: | L. Moizo, J.-P. Laigneau, S. Levasseur, M. J. M. Lewin, André Bado, Florence Reyl-Desmars |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
Agonist
medicine.medical_specialty DNA Complementary Tetrahydronaphthalenes Physiology medicine.drug_class Adrenergic beta-Antagonists Biology Rats Sprague-Dawley chemistry.chemical_compound Physiology (medical) Internal medicine Gastrins Receptors Adrenergic beta Pyloric Antrum medicine Animals Beta (finance) Antrum Gastrin Hepatology SR 59230A Gastroenterology Antagonist Adrenergic beta-Agonists Rats Dissociation constant Endocrinology Somatostatin chemistry Pindolol Female |
| Zdroj: | American Journal of Physiology-Gastrointestinal and Liver Physiology. 272:G1000-G1006 |
| ISSN: | 1522-1547 0193-1857 |
| Popis: | The beta 3-adrenoceptor (beta 3-AR) agonist SR-58611A inverted question markethyl-[(7s)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]5, 6,7,8-tetrahydronaphth-2-yl]oxyacetate hydrochloride inverted question mark stimulated somatostatin and gastrin releases in isolated rat gastric antral epithelial cells. Stimulation was a concentration-dependent process with 50% effective concentrations of 2.7 +/- 1.1 and 3.8 +/- 1.9 nM compared with 209 +/- 71 and 230 +/- 51 nM for isoproterenol, respectively. It was inhibited by selective beta-AR antagonists with the following rank order of potency: SR-59230A 3-(2-ethylphenoxy)1-[(1S)-1,2,3,4-tetrahydronaphth- 1-ylamino]-(2S)-2-propranol oxalate; beta 3-AR antagonist > ICI-118551[erythro-(+/-)-1-(7-methylindan-4-yloxy)-3- isopropylaminobutan-2-ol-hydrochloride; beta 2-AR antagonist > CGP-20712A[(+/-)-[2-(3-carbarmoyl-4-hydroxyphenoxy)-et hyl- amino]-3-[4 (1-methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy]- 2-propranol; beta 1-AR antagonist]. Furthermore, specific binding of 125I-cyanopindolol to the isolated cells was demonstrated and was displaced by the beta-AR antagonists according to the same rank order of potency and with apparent dissociation constants consistent with the 50% inhibitory concentrations for SR-58611A-stimulated somatostatin and gastrin releases. In addition, the presence of beta 3-AR mRNA was detected by reverse transcriptase polymerase chain reaction. These findings provide the first evidence for a gastric beta 3-AR mediating catecholamine stimulation of gastrin and somatostatin releases from antral cells. |
| Databáze: | OpenAIRE |
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