Literature DB >> 10340609

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

T L Shih1, 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.   

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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Year:  1999        PMID: 10340609     DOI: 10.1016/s0960-894x(99)00182-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Characterization of beta3-adrenergic receptor: determination of pharmacophore and 3D QSAR model for beta3 adrenergic receptor agonism.

Authors:  Philip Prathipati; Anil K Saxena
Journal:  J Comput Aided Mol Des       Date:  2005-02       Impact factor: 3.686

2.  2-(1,3-Dioxoisoindolin-2-yl)acetonitrile.

Authors:  Younas Aouine; Anouar Alami; Abdelilah El Hallaoui; Abdelrhani Elachqar; Hafid Zouihri
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-09-25

3.  Pharmacophore-guided Virtual Screening to Identify New β3 -adrenergic Receptor Agonists.

Authors:  Navista Sri Octa Ujiantari; Seungmin Ham; Chisae Nagiri; Wataru Shihoya; Osamu Nureki; Dana Sabine Hutchinson; Daniela Schuster
Journal:  Mol Inform       Date:  2022-02-02       Impact factor: 4.050

  3 in total

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