Murine ventricular L-type Ca(2+) current is enhanced by zinterol via beta(1)-adrenoceptors, and is reduced in TG4 mice overexpressing the human beta(2)-adrenoceptor

Br J Pharmacol. 2001 May;133(1):73-82. doi: 10.1038/sj.bjp.0704045.

Abstract

1. The functional coupling of beta(2)-adrenoceptors (beta(2)-ARs) to murine L-type Ca(2+) current (I(Ca(L))) was investigated with two different approaches. The beta(2)-AR signalling cascade was activated either with the beta(2)-AR selective agonist zinterol (myocytes from wild-type mice), or by spontaneously active, unoccupied beta(2)-ARs (myocytes from TG4 mice with 435 fold overexpression of human beta(2)-ARs). Ca(2+) and Ba(2+) currents were recorded in the whole-cell and cell-attached configuration of the patch-clamp technique, respectively. 2. Zinterol (10 microM) significantly increased I(Ca(L)) amplitude of wild-type myocytes by 19+/-5%, and this effect was markedly enhanced after inactivation of Gi-proteins with pertussis-toxin (PTX; 76+/-13% increase). However, the effect of zinterol was entirely mediated by the beta(1)-AR subtype, since it was blocked by the beta(1)-AR selective antagonist CGP 20712A (300 nM). The beta(2)-AR selective antagonist ICI 118,551 (50 nM) did not affect the response of I(Ca(L)) to zinterol. 3. In myocytes with beta(2)-AR overexpression I(Ca(L)) was not stimulated by the activated signalling cascade. On the contrary, I(Ca(L)) was lower in TG4 myocytes and a significant reduction of single-channel activity was identified as a reason for the lower whole-cell I(Ca(L)). The beta(2)-AR inverse agonist ICI 118,551 did not further decrease I(Ca(L)). PTX-treatment increased current amplitude to values found in control myocytes. 4. In conclusion, there is no evidence for beta(2)-AR mediated increases of I(Ca(L)) in wild-type mouse ventricular myocytes. Inactivation of Gi-proteins does not unmask beta(2)-AR responses to zinterol, but augments beta(1)-AR mediated increases of I(Ca(L)). In the mouse model of beta(2)-AR overexpression I(Ca(L)) is reduced due to tonic activation of Gi-proteins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-1 Receptor Agonists
  • Adrenergic beta-2 Receptor Agonists
  • Adrenergic beta-Agonists / pharmacology*
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Barium / metabolism
  • Binding Sites
  • Calcium / metabolism
  • Calcium Channels, L-Type / metabolism*
  • Electric Conductivity
  • Ethanolamines / pharmacology*
  • GTP-Binding Protein alpha Subunits, Gi-Go / metabolism
  • Heart Ventricles / cytology
  • Heart Ventricles / drug effects*
  • Heart Ventricles / metabolism
  • Humans
  • Imidazoles / pharmacology
  • Ion Channel Gating / drug effects
  • Isoproterenol / antagonists & inhibitors
  • Isoproterenol / pharmacology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Myocardium / cytology
  • Myocardium / metabolism
  • Pertussis Toxin
  • Propanolamines / pharmacology
  • Protein Binding
  • Receptors, Adrenergic, beta-1 / metabolism*
  • Receptors, Adrenergic, beta-2 / genetics
  • Receptors, Adrenergic, beta-2 / metabolism*
  • Virulence Factors, Bordetella / pharmacology

Substances

  • Adrenergic beta-1 Receptor Agonists
  • Adrenergic beta-2 Receptor Agonists
  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Calcium Channels, L-Type
  • Ethanolamines
  • Imidazoles
  • Propanolamines
  • Receptors, Adrenergic, beta-1
  • Receptors, Adrenergic, beta-2
  • Virulence Factors, Bordetella
  • Barium
  • ICI 118551
  • zinterol
  • CGP 20712A
  • Pertussis Toxin
  • GTP-Binding Protein alpha Subunits, Gi-Go
  • Isoproterenol
  • Calcium