Literature DB >> 11055339

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.

E R Parmee1, L L Brockunier, J He, S B Singh, M R Candelore, M A Cascieri, L Deng, Y Liu, L Tota, M J Wyvratt, M H Fisher, A E Weber.   

Abstract

Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (beta3 EC50 = 78 nM) did not activate the beta1 and beta2 ARs at 10 microM, and showed >1000-fold selectivity over binding to the beta1 and beta2 ARs.

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Year:  2000        PMID: 11055339     DOI: 10.1016/s0960-894x(00)00459-5

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


  4 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.  N-(2,5-Dimethoxy-phen-yl)-4-nitro-benzene-sulfonamide.

Authors:  Guo-Yao Zhang; Shan Qian; Xiao-Cen Li; Yong Wu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-07-22

3.  Signaling pathways mediating beta3-adrenergic receptor-induced production of interleukin-6 in adipocytes.

Authors:  Inna E Tchivileva; Kai Soo Tan; Maria Gambarian; Andrea G Nackley; Alexander V Medvedev; Sergei Romanov; Patrick M Flood; William Maixner; Sergei S Makarov; Luda Diatchenko
Journal:  Mol Immunol       Date:  2009-05-23       Impact factor: 4.407

4.  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

  4 in total

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