title: Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
abstract: A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(2)- or beta(3)-AR.
authors.affiliation: Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. robert_l_dow@groton.pfizer.com
authors.forename: Robert L
authors.initials: RL
authors.lastname: Dow
authors.forename: Ernest S
authors.initials: ES
authors.lastname: Paight
authors.forename: Steven R
authors.initials: SR
authors.lastname: Schneider
authors.forename: John R
authors.initials: JR
authors.lastname: Hadcock
authors.forename: Diane M
authors.initials: DM
authors.lastname: Hargrove
authors.forename: Kelly A
authors.initials: KA
authors.lastname: Martin
authors.forename: Tristan S
authors.initials: TS
authors.lastname: Maurer
authors.forename: Nancy A
authors.initials: NA
authors.lastname: Nardone
authors.forename: David A
authors.initials: DA
authors.lastname: Tess
authors.forename: Paul
authors.initials: P
authors.lastname: DaSilva-Jardine
mesh_terms: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D006801:Humans; D010101:Oxygen Consumption / Q000187:drug effects / Q000502:physiology; D051381:Rats; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013449:Sulfonamides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D022702:Receptors, Adrenergic, beta-3; D013449:Sulfonamides