L-770,644: A potent and selective human β3 adrenergic receptor agonist with improved oral bioavailability

Article abstract of DOI:10.1016/S0960-894X(99)00182-1

L-770,644 (9c) is a potent and selective agonist of the human β3 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.