title: L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: T L
authors.initials: TL
authors.lastname: Shih
authors.forename: M R
authors.initials: MR
authors.lastname: Candelore
authors.forename: M A
authors.initials: MA
authors.lastname: Cascieri
authors.forename: S H
authors.initials: SH
authors.lastname: Chiu
authors.forename: L F
authors.initials: LF
authors.lastname: Colwell
authors.forename: L
authors.initials: L
authors.lastname: Deng
authors.forename: W P
authors.initials: WP
authors.lastname: Feeney
authors.forename: M J
authors.initials: MJ
authors.lastname: Forrest
authors.forename: G J
authors.initials: GJ
authors.lastname: Hom
authors.forename: D E
authors.initials: DE
authors.lastname: MacIntyre
authors.forename: R R
authors.initials: RR
authors.lastname: Miller
authors.forename: R A
authors.initials: RA
authors.lastname: Stearns
authors.forename: C D
authors.initials: CD
authors.lastname: Strader
authors.forename: L
authors.initials: L
authors.lastname: Tota
authors.forename: M J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
authors.forename: A E
authors.initials: AE
authors.lastname: Weber
mesh_terms: D000284:Administration, Oral; D000318:Adrenergic beta-Agonists / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D001682:Biological Availability; D004285:Dogs; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D051381:Rats; D013449:Sulfonamides / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000494:pharmacology*; D013777:Tetrazoles / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000318:Adrenergic beta-Agonists; D013449:Sulfonamides; D013777:Tetrazoles; C120629:L 770644