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Molecular Pharmacology

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Research ArticleArticle

(−)-CGP 12177 Causes Cardiostimulation and Binds to Cardiac Putative β4-Adrenoceptors in Both Wild-Type and β3-Adrenoceptor Knockout Mice

Alberto J. Kaumann, Frédéric Preitner, Doreen Sarsero, Peter Molenaar, Jean-Pierre Revelli and Jean Paul Giacobino
Molecular Pharmacology April 1998, 53 (4) 670-675; DOI: https://doi.org/10.1124/mol.53.4.670
Alberto J. Kaumann
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Frédéric Preitner
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Doreen Sarsero
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Peter Molenaar
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Jean-Pierre Revelli
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Jean Paul Giacobino
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Abstract

Some blockers of β1- and β2-adrenoceptors cause cardiostimulant effects through an atypical β-adrenoceptor (putative β4-adrenoceptor) that resembles the β3-adrenoceptor. It is likely but not proven that the putative β4-adrenoceptor is genetically distinct from the β3-adrenoceptor. We therefore investigated whether or not the cardiac atypical β-adrenoceptor could mediate agonist effects in mice lacking a functional β3-adrenoceptor gene (β3KO). (−)-CGP 12177, a β1- and β2-adrenoceptor blocker that causes agonist effects through both β3-adrenoceptors and cardiac putative β4-adrenoceptors, caused cardiostimulant effects that were not different in atria from wild-type (WT) mice and β3KO mice. The effects of (−)-CGP 12177 were resistant to blockade by (−)-propranolol (200 nm) but were blocked by (−)-bupranolol (1 μm) with an equilibrium dissociation constant of 15 nm in WT and 17 nmin β3KO. (−)-[3H]CGP 12177 labeled a similar density of the putative β4-adrenoceptor in ventricular membranes from the hearts of both WT (B max = 52 fmol/mg protein) and β3KO (B max = 53 fmol/mg protein) mice. The affinity of (−)-[3H]CGP 12177 for the cardiac putative β4-adrenoceptor was not different between WT (K d = 46 nm) and β3KO (K d= 40 nm). These results provide definitive evidence that the cardiac putative β4-adrenoceptor is distinct from the β3-adrenoceptor.

Footnotes

    • Received December 11, 1997.
    • Accepted January 12, 1998.
  • Send reprint requests to: Dr. A. J. Kaumann, The Babraham Institute, Cambridge CB2 4AT, England. E-mail:alberto.kaumann{at}bbsrc.ac.uk

  • This work was supported by the British Heart Foundation (A.J.K.) and by a Senior Research Fellowship (P.M.) at the National Health and Medical Research Council of Australia.

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 53 (4)
Molecular Pharmacology
Vol. 53, Issue 4
1 Apr 1998
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Research ArticleArticle

(−)-CGP 12177 Causes Cardiostimulation and Binds to Cardiac Putative β4-Adrenoceptors in Both Wild-Type and β3-Adrenoceptor Knockout Mice

Alberto J. Kaumann, Frédéric Preitner, Doreen Sarsero, Peter Molenaar, Jean-Pierre Revelli and Jean Paul Giacobino
Molecular Pharmacology April 1, 1998, 53 (4) 670-675; DOI: https://doi.org/10.1124/mol.53.4.670

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Research ArticleArticle

(−)-CGP 12177 Causes Cardiostimulation and Binds to Cardiac Putative β4-Adrenoceptors in Both Wild-Type and β3-Adrenoceptor Knockout Mice

Alberto J. Kaumann, Frédéric Preitner, Doreen Sarsero, Peter Molenaar, Jean-Pierre Revelli and Jean Paul Giacobino
Molecular Pharmacology April 1, 1998, 53 (4) 670-675; DOI: https://doi.org/10.1124/mol.53.4.670
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