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L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Shih, T L; Candelore, M R; Cascieri, M A; Chiu, S H; Colwell, L F; Deng, L; Feeney, W P; Forrest, M J; Hom, G J; MacIntyre, D E; Miller, R R; Stearns, R A; Strader, C D; Tota, L; Wyvratt, M J; Fisher, M H; Weber, A E.
Affiliation
  • Shih TL; Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett ; 9(9): 1251-4, 1999 May 03.
Article in En | MEDLINE | ID: mdl-10340609
ABSTRACT
L-770,644 (9c) is a potent and selective agonist of the human beta3 adrenergic receptor (EC50 = 13 nM). It shows good oral bioavailability in both dogs and rats (%F = 27), and is a full agonist for glycerolemia in the rhesus monkey (ED50 = 0.21 mg/kg). Based on its desirable in vitro and in vivo properties, L-770,644 was chosen for further preclinical evaluation.
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Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Tetrazoles / Adrenergic beta-Agonists Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 1999 Document type: Article Affiliation country: United States
Search on Google
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PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Tetrazoles / Adrenergic beta-Agonists Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 1999 Document type: Article Affiliation country: United States