title: BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
abstract: A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(3) full agonist (K(i)=21 nM, 95% activation) with partial agonist (45%) activity at the beta(1) receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ashvinikumar.gavai@bms.com
authors.forename: A V
authors.initials: AV
authors.lastname: Gavai
authors.forename: P M
authors.initials: PM
authors.lastname: Sher
authors.forename: A B
authors.initials: AB
authors.lastname: Mikkilineni
authors.forename: K M
authors.initials: KM
authors.lastname: Poss
authors.forename: P J
authors.initials: PJ
authors.lastname: McCann
authors.forename: R N
authors.initials: RN
authors.lastname: Girotra
authors.forename: L G
authors.initials: LG
authors.lastname: Fisher
authors.forename: G
authors.initials: G
authors.lastname: Wu
authors.forename: M S
authors.initials: MS
authors.lastname: Bednarz
authors.forename: A
authors.initials: A
authors.lastname: Mathur
authors.forename: T C
authors.initials: TC
authors.lastname: Wang
authors.forename: C Q
authors.initials: CQ
authors.lastname: Sun
authors.forename: D A
authors.initials: DA
authors.lastname: Slusarchyk
authors.forename: S
authors.initials: S
authors.lastname: Skwish
authors.forename: G T
authors.initials: GT
authors.lastname: Allen
authors.forename: D E
authors.initials: DE
authors.lastname: Hillyer
authors.forename: B H
authors.initials: BH
authors.lastname: Frohlich
authors.forename: B E
authors.initials: BE
authors.lastname: Abboa-Offei
authors.forename: M
authors.initials: M
authors.lastname: Cap
authors.forename: T L
authors.initials: TL
authors.lastname: Waldron
authors.forename: R J
authors.initials: RJ
authors.lastname: George
authors.forename: B
authors.initials: B
authors.lastname: Tesfamariam
authors.forename: T W
authors.initials: TW
authors.lastname: Harper
authors.forename: C P
authors.initials: CP
authors.lastname: Ciosek
authors.forename: D A
authors.initials: DA
authors.lastname: Young
authors.forename: K E
authors.initials: KE
authors.lastname: Dickinson
authors.forename: A A
authors.initials: AA
authors.lastname: Seymour
authors.forename: C M
authors.initials: CM
authors.lastname: Arbeeny
authors.forename: W N
authors.initials: WN
authors.lastname: Washburn
mesh_terms: D000284:Administration, Oral; D000322:Adrenergic Agonists / Q000737:chemistry* / Q000494:pharmacology*; D058665:Adrenergic beta-1 Receptor Agonists; D058667:Adrenergic beta-3 Receptor Agonists; D000813:Anilides / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002522:Chlorocebus aethiops; D004353:Drug Evaluation, Preclinical; D005227:Fatty Acids / Q000097:blood; D006801:Humans; D051379:Mice; D008820:Mice, Obese; D018342:Receptors, Adrenergic, beta-1 / Q000378:metabolism; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000322:Adrenergic Agonists; D058665:Adrenergic beta-1 Receptor Agonists; D058667:Adrenergic beta-3 Receptor Agonists; D000813:Anilides; D001786:Blood Glucose; D005227:Fatty Acids; D018342:Receptors, Adrenergic, beta-1; D022702:Receptors, Adrenergic, beta-3; C448380:BMS-196085