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. 2000 Jul 3;10(13):1427-9.
doi: 10.1016/s0960-894x(00)00267-5.

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist

D D Feng  1 , T Biftu, M R Candelore, M A Cascieri, L F Colwell Jr, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, R R Miller, R A Stearns, C D Strader, L Tota, M J Wyvratt, M H Fisher, A E Weber
Affiliations

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist

D D Feng et al. Bioorg Med Chem Lett. .

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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