Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides

Autor: Elizabeth M. Naylor, D. Euan MacIntyre, Liping Deng, Catherine D. Strader, Michael H. Fisher, Margaret A. Cascieri, Lawrence F. Colwell, William P. Feeney, Ann E. Weber, Pei-Ran Wang, Mari R. Candelore, Gary J Hom, Linda Brockunier, Laurie Tota, Michael J. Forrest, Vincent J. Colandrea, Emma R. Parmee, Matthew J. Wyvratt, Leroy Perkins
Rok vydání: 1999
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 9(5)
ISSN: 0960-894X
Popis: The 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.
Databáze: OpenAIRE
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