title: Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
abstract: The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors: E M
authors: EM
authors: Naylor
authors: E R
authors: ER
authors: Parmee
authors: V J
authors: VJ
authors: Colandrea
authors: L
authors: L
authors: Perkins
authors: L
authors: L
authors: Brockunier
authors: M R
authors: MR
authors: Candelore
authors: M A
authors: MA
authors: Cascieri
authors: L F
authors: LF
authors: Colwell
authors: L
authors: L
authors: Deng
authors: W P
authors: WP
authors: Feeney
authors: M J
authors: MJ
authors: Forrest
authors: G J
authors: GJ
authors: Hom
authors: D E
authors: DE
authors: MacIntyre
authors: C D
authors: CD
authors: Strader
authors: L
authors: L
authors: Tota
authors: P R
authors: PR
authors: Wang
authors: M J
authors: MJ
authors: Wyvratt
authors: M H
authors: MH
authors: Fisher
authors: A E
authors: AE
authors: Weber
mesh_terms: D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D008253:Macaca mulatta; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism*; D022702:Receptors, Adrenergic, beta-3; D013329:Structure-Activity Relationship
chemical_list: D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D003517:Cyclopentanes; D007093:Imidazoles; D011943:Receptors, Adrenergic, beta; D022702:Receptors, Adrenergic, beta-3; C119127:cyclopentylpropylimidazolidinone