Bioorganic and Medicinal Chemistry Letters p. 1251 - 1254 (1999)
Update date:2022-08-05
Topics:
Shih, Thomas L.
Candelore, Mari R.
Cascieri, Margaret A.
Chiu, Shuet-Hing L.
Colwell Jr., Lawrence F.
Deng, Liping
Feeney, William P.
Forrest, Michael J.
Hom, Gary J.
Macintyre, D. Euan
Miller, Randall R.
Stearns, Ralph A.
Strader, Catherine D.
Tota, Laurie
Wyvratt, Matthew J.
Fisher, Michael H.
Weber, Ann E.
L-770,644 (9c) is a potent and selective agonist of the human β3 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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