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L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability. |
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| Authors: | T L Shih M R Candelore M A Cascieri S H Chiu L F Colwell L Deng W P Feeney M J Forrest G J Hom D E MacIntyre R R Miller R A Stearns C D Strader L Tota M J Wyvratt M H Fisher A E Weber |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. |
| 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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