title: Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.
abstract: A study of 4-acylaminobenzenesulfonamides in a cloned human beta 3 adrenergic receptor assay resulted in the discovery of n-hexylurea, L-755,507 (22). This 0.43 nM beta 3 agonist, which is > 440-fold selective over both beta 1 and beta 2 binding, is among the most potent human beta 3 agonists reported to date.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
authors.forename: E R
authors.initials: ER
authors.lastname: Parmee
authors.forename: H O
authors.initials: HO
authors.lastname: Ok
authors.forename: M R
authors.initials: MR
authors.lastname: Candelore
authors.forename: L
authors.initials: L
authors.lastname: Tota
authors.forename: L
authors.initials: L
authors.lastname: Deng
authors.forename: C D
authors.initials: CD
authors.lastname: Strader
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* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D008968:Molecular Conformation; D015394:Molecular Structure; D011943:Receptors, Adrenergic, beta / Q000187:drug effects* / Q000502:physiology; D018342:Receptors, Adrenergic, beta-1 / Q000187:drug effects; D018343:Receptors, Adrenergic, beta-2 / Q000187:drug effects; D022702:Receptors, Adrenergic, beta-3; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000318:Adrenergic beta-Agonists; C112650:L 755507; D011943:Receptors, Adrenergic, beta; D018342:Receptors, Adrenergic, beta-1; D018343:Receptors, Adrenergic, beta-2; D022702:Receptors, Adrenergic, beta-3; D013449:Sulfonamides