Literature DB >> 8180506

Studies on the intrinsic activity (efficacy) of human adrenergic receptors. Co-expression of beta 1 and beta 2 reveals a lower efficacy for the beta 1 receptor.

L Birnbaumer1, F O Levy, X Zhu, A J Kaumann.   

Abstract

Through co-expression of the human beta 1 and beta 2 adrenergic receptors in a single tester cell (the murine L fibroblast) and through assaying the effect of the beta 1 and beta 2 selective blockers CGP 20712A and ICI 118551 on isoproterenol-stimulated adenylyl cyclase, it is shown that the maximal stimulation achievable with a given cell density of beta 1 adrenergic receptor is less than that obtained with the same density of the beta 2 adrenergic receptor. It is concluded that the efficacy of the 2 receptors differs in that the beta 1 adrenergic receptor has a lower efficacy (or intrinsic activity) than does the beta 2 adrenergic receptor.

Entities:  

Mesh：

Substances：

Year:  1994        PMID： 8180506      PMCID： PMC325127     

Source DB:  PubMed          Journal:  Tex Heart Inst J        ISSN： 0730-2347


  12 in total

1.  A highly sensitive adenylate cyclase assay.

Authors:  Y Salomon; C Londos; M Rodbell
Journal:  Anal Biochem       Date:  1974-04       Impact factor: 3.365

2.  The human heart beta-adrenergic receptors. II. Coupling of beta 2-adrenergic receptors with the adenylate cyclase system.

Authors:  M Waelbroeck; G Taton; M Delhaye; P Chatelain; J C Camus; R Pochet; J L Leclerc; J M De Smet; P Robberecht; J Christophe
Journal:  Mol Pharmacol       Date:  1983-09       Impact factor: 4.436

3.  A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

Authors:  P Samama; S Cotecchia; T Costa; R J Lefkowitz
Journal:  J Biol Chem       Date:  1993-03-05       Impact factor: 5.157

4.  Guanine nucleotide and magnesium ion regulation of the interaction of gonadotropic and beta-adrenergic receptors with their hormones: a comparative study using a single membrane system.

Authors:  J Abramowitz; R Iyengar; L Birnbaumer
Journal:  Endocrinology       Date:  1982-02       Impact factor: 4.736

5.  Development and characterization of a mouse cell line expressing the human V2 vasopressin receptor gene.

Authors:  M Birnbaumer; V Hinrichs; A P Themmen; A P Themen
Journal:  Mol Endocrinol       Date:  1990-02

6.  Coexistence of functioning beta 1- and beta 2-adrenoceptors in single myocytes from human ventricle.

Authors:  F del Monte; A J Kaumann; P A Poole-Wilson; D G Wynne; J Pepper; S E Harding
Journal:  Circulation       Date:  1993-09       Impact factor: 29.690

7.  Hormone-stimulated desensitization of hormone-dependent adenylyl cyclase. Dual action of luteninizing hormone on pig graafian follicle membranes.

Authors:  J Bockaert; M Hunzicker-Dunn; L Birnbaumer
Journal:  J Biol Chem       Date:  1976-05-10       Impact factor: 5.157

8.  Beta 1- and beta 2-adrenergic receptors display subtype-selective coupling to Gs.

Authors:  S A Green; B D Holt; S B Liggett
Journal:  Mol Pharmacol       Date:  1992-05       Impact factor: 4.436

9.  Beta 2-adrenoceptor-mediated positive inotropic effect of adrenaline in human ventricular myocardium. Quantitative discrepancies with binding and adenylate cyclase stimulation.

Authors:  A J Kaumann; H Lemoine
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-04       Impact factor: 3.000

10.  Molecular cloning of a human gene (S31) encoding a novel serotonin receptor mediating inhibition of adenylyl cyclase.

Authors:  F O Levy; T Gudermann; M Birnbaumer; A J Kaumann; L Birnbaumer
Journal:  FEBS Lett       Date:  1992-01-20       Impact factor: 4.124
View more
  4 in total

Review 1.  Activation of G-proteins in brain by endogenous and exogenous cannabinoids.

Authors:  Steven R Childers
Journal:  AAPS J       Date:  2006-03-10       Impact factor: 4.009

Review 2.  Discovery of new GPCR biology: one receptor structure at a time.

Authors:  Michael A Hanson; Raymond C Stevens
Journal:  Structure       Date:  2009-01-14       Impact factor: 5.006

3.  Preclinical characterization of a novel radiolabeled analog of practolol for the molecular imaging of myocardial β-adrenoceptor density.

Authors:  Eric Carbonnelle; Véronique Josserand; Laurent M Riou; Olivier Ormezzano; Alexis Broisat; Pascale Perret; Gilles Barone-Rochette; Daniel Fagret; Catherine Ghezzi
Journal:  J Nucl Cardiol       Date:  2014-05-30       Impact factor: 5.952

4.  The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.

Authors:  Veli-Pekka Jaakola; Mark T Griffith; Michael A Hanson; Vadim Cherezov; Ellen Y T Chien; J Robert Lane; Adriaan P Ijzerman; Raymond C Stevens
Journal:  Science       Date:  2008-10-02       Impact factor: 47.728
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.