| Literature DB >> 9873496 |
A E Weber1, H O Ok, R F Alvaro, M R Candelore, M A Cascieri, S H Chiu, L Deng, M J Forrest, G J Hom, J E Hutchins, J Kao, D E MacIntyre, R J Mathvink, D McLoughlin, R R Miller, R C Newbold, T V Olah, E R Parmee, L Perkins, R A Stearns, C D Strader, J Szumiloski, Y S Tang, L Tota, M H Fisher.
Abstract
Pyridyloxypropanolamines L-749,372 (8, beta 3 EC50 = 3.6 nM) and L-750,355 (29, beta 3 EC50 = 13 nM) are selective partial agonists of the human receptor, with 33% and 49% activation, respectively. Both stimulate lipolysis in rhesus monkeys (ED50 = 2 and 0.8 mg/kg, respectively), with minimal effects on heart rate. Oral bioavailability in dogs, 41% for L-749,372 and 47% for L-750,355, is improved relative to phenol analogs.Entities:
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Year: 1998 PMID： 9873496 DOI： 10.1016/s0960-894x(98)00381-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823