Human β3 andrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides

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Abstract

The cyclopentylpropylimidazolidinone L-766,892 is a potent β3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the β1 and β2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.

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Present address: Schering Plough Research Institute, Kenilworth, NJ 07033, U.S.A.

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