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3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists |
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| Authors: | EM Naylor VJ Colandrea MR Candelore MA Cascieri LF Colwell L Deng WP Feeney MJ Forrest GJ Hom DE MacIntyre CD Strader L Tota PR Wang MJ Wyvratt MH Fisher AE Weber |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA. |
| Abstract: | The 3-pyridylethanolamine L-757,793 is a potent beta 3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta 1 and beta 2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol. |
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