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ID: ALA1132038
Journal: Bioorg Med Chem Lett
Title: L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Authors: Shih TL, Candelore MR, Cascieri MA, Chiu SH, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
Abstract: L-770,644 (9c) is a potent and selective agonist of the human beta3 adrenergic receptor (EC50 = 13 nM). It shows good oral bioavailability in both dogs and rats (%F = 27), and is a full agonist for glycerolemia in the rhesus monkey (ED50 = 0.21 mg/kg). Based on its desirable in vitro and in vivo properties, L-770,644 was chosen for further preclinical evaluation.
CiteXplore: 10340609