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Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides |
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| Authors: | Naylor E M Parmee E R Colandrea V J Perkins L Brockunier L Candelore M R Cascieri M A Colwell L F Deng L Feeney W P Forrest M J Hom G J MacIntyre D E Strader C D Tota L Wang P R Wyvratt M J Fisher M H Weber A E |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. |
| Abstract: | 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. |
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