Literature DB >> 10201842

Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.

E M Naylor1, E R Parmee, V J Colandrea, L Perkins, L Brockunier, M R Candelore, M A Cascieri, L F Colwell, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, C D Strader, L Tota, P R Wang, M J Wyvratt, M H Fisher, A E Weber.   

Abstract

The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.

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Year:  1999        PMID: 10201842     DOI: 10.1016/s0960-894x(99)00072-4

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


  2 in total

1.  Prototropic tautomerism of imidazolone in aqueous solution: a density functional approach using the combined discrete/self-consistent reaction field (SCRF) models.

Authors:  Yi Ren; Ming Li; Ning-Bew Wong
Journal:  J Mol Model       Date:  2005-03-03       Impact factor: 1.810

2.  Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.

Authors:  P Senthil Kumar; Prasad V Bharatam
Journal:  Med Chem Res       Date:  2009-10-31       Impact factor: 1.965

  2 in total

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