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    Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54.

    Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

    Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

    Source

    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

    Abstract

    Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 EC50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs.

    PMID:
    10201841
    [PubMed - indexed for MEDLINE]

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