Beta3-adrenergic relaxation of bovine iris sphincter

FEBS Letters
O GeyerY Oron

Abstract

Bovine iris sphincter in vitro responded to beta-adrenergic stimulation with pronounced relaxation (EC50 of isoproterenol = 0.3 nM), which was potentiated by the cAMP phosphodiesterase inhibitor, isobutylmethylxanthine, and mimicked by the adenylyl cyclase activator, forskolin. The beta1/beta2 antagonist, propranolol, exhibited low potency with calculated Ki of 200 nM. The beta3-selective antagonist, bupranolol, exhibited a biphasic inhibition profile, with calculated Kis of approximately 20-50 and 200-300 nM. The beta3-selective agonist, BRL 37344, elicited 70% of maximal relaxation (EC50 = 30 nM). When relaxation was induced by BRL 37344, bupranolol exhibited much higher potency (calculated Ki = 1 nM). Our data suggest that the beta-adrenergic relaxation response in bovine iris sphincter is mediated by a mixed population of beta-adrenergic receptors, with a predominant contribution of atypical, most likely beta3 subtype, receptors.

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Citations

Jan 25, 2013·Naunyn-Schmiedeberg's Archives of Pharmacology·Adrian GerickeMartin C Michel
Sep 27, 2001·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·N A SharifT L Davis
Apr 17, 2013·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Gary D NovackNancy E Martin
Mar 18, 2011·Expert Opinion on Therapeutic Patents·Maria Grazia Perrone, Antonio Scilimati
Feb 12, 2011·Acta Ophthalmologica·Chris C JanbazAnders Behndig
Mar 25, 2005·Toxicological Sciences : an Official Journal of the Society of Toxicology·Paul A DabischSandra A Thomson
Jul 10, 2021·Investigative Ophthalmology & Visual Science·Murat Topcuoglu, Fatih Aslan

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