Human β3 andrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides
摘要:
The cyclopentylpropylimidazolidinone L-766,892 is a potent beta(3) AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta(1) and beta(2) ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate. (C) 1999 Elsevier Science Ltd. All rights reserved.