Human β3 andrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides
1999; Elsevier BV; Volume: 9; Issue: 5 Linguagem: Inglês
10.1016/s0960-894x(99)00072-4
ISSN1464-3405
AutoresElizabeth M. Naylor, Emma R. Parmee, Vincent J. Colandrea, Leroy Perkins, Linda Brockunier, Mari R. Candelore, Margaret A. Cascieri, Lawrence F. Colwell, Liping Deng, William P. Feeney, Michael J. Forrest, Gary J. Hom, D. Euan MacIntyre, Catherine D. Strader, Laurie Tota, Pei-Ran Wang, Matthew J. Wyvratt, Michael H. Fisher, Ann E. Weber,
Tópico(s)Pharmacological Effects and Assays
ResumoThe cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 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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