title: 3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
abstract: The 3-pyridylethanolamine L-757,793 is a potent beta 3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta 1 and beta 2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
authors.forename: E M
authors.initials: EM
authors.lastname: Naylor
authors.forename: V J
authors.initials: VJ
authors.lastname: Colandrea
authors.forename: M R
authors.initials: MR
authors.lastname: Candelore
authors.forename: M A
authors.initials: MA
authors.lastname: Cascieri
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: C D
authors.initials: CD
authors.lastname: Strader
authors.forename: L
authors.initials: L
authors.lastname: Tota
authors.forename: P R
authors.initials: PR
authors.lastname: Wang
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: D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004285:Dogs; D006801:Humans; D008253:Macaca mulatta; D008297:Male; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D022702:Receptors, Adrenergic, beta-3; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000318:Adrenergic beta-Agonists; C112650:L 755507; D011943:Receptors, Adrenergic, beta; D022702:Receptors, Adrenergic, beta-3; D013449:Sulfonamides