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Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist |
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| Authors: | Feng D D Biftu T Candelore M R Cascieri M A Colwell L F Deng L Feeney W P Forrest M J Hom G J MacIntyre D E Miller R R Stearns R A Strader C D Tota L Wyvratt M J Fisher M H Weber A E |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, USA. danqing_feng@merck.com |
| Abstract: | 5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta3 adrenergic receptor agonist (beta3 EC50 = 23 nM, beta1 IC50 = 3000 nM, beta2 IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable beta3 adrenergic receptor agonists reported to date. |
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