Transgenic simulation of human heart failure-like L-type Ca2+-channels: implications for fibrosis and heart rate in mice

Cardiovasc Res. 2009 Dec 1;84(3):396-406. doi: 10.1093/cvr/cvp251. Epub 2009 Jul 20.

Abstract

Aims: Cardiac L-type Ca(2+)-currents show distinct alterations in chronic heart failure, including increased single-channel activity and blunted adrenergic stimulation, but minor changes of whole-cell currents. Expression of L-type Ca(2+)-channel beta(2)-subunits is enhanced in human failing hearts. In order to determine whether prolonged alteration of Ca(2+)-channel gating by beta(2)-subunits contributes to heart failure pathogenesis, we generated and characterized transgenic mice with cardiac overexpression of a beta(2a)-subunit or the pore Ca(v)1.2 or both, respectively.

Methods and results: Four weeks induction of cardiac-specific overexpression of rat beta(2a)-subunits shifted steady-state activation and inactivation of whole-cell currents towards more negative potentials, leading to increased Ca(2+)-current density at more negative test potentials. Activity of single Ca(2+)-channels was increased in myocytes isolated from beta(2a)-transgenic mice. Ca(2+)-current stimulation by 8-Br-cAMP and okadaic acid was blunted in beta(2a)-transgenic myocytes. In vivo investigation revealed hypotension and bradycardia upon Ca(v)1.2-transgene expression but not in mice only overexpressing beta(2a). Double-transgenics showed cardiac arrhythmia. Interstitial fibrosis was aggravated by the beta(2a)-transgene compared with Ca(v)1.2-transgene expression alone. Overt cardiac hypertrophy was not observed in any model.

Conclusion: Cardiac overexpression of a Ca(2+)-channel beta(2a)-subunit alone is sufficient to induce Ca(2+)-channel properties characteristic of chronic human heart failure. beta(2a)-overexpression by itself did not induce cardiac hypertrophy or contractile dysfunction, but aggravated the development of arrhythmia and fibrosis in Ca(v)1.2-transgenic mice.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Bromo Cyclic Adenosine Monophosphate / pharmacology
  • Animals
  • Arrhythmias, Cardiac / metabolism
  • Arrhythmias, Cardiac / pathology
  • Arrhythmias, Cardiac / physiopathology
  • Calcium Channels, L-Type / drug effects
  • Calcium Channels, L-Type / genetics
  • Calcium Channels, L-Type / metabolism*
  • Chronic Disease
  • Disease Models, Animal
  • Fibrosis
  • Heart Failure / metabolism*
  • Heart Failure / pathology*
  • Heart Failure / physiopathology
  • Heart Rate / physiology*
  • Humans
  • Mice
  • Mice, Transgenic
  • Myocardial Contraction / physiology
  • Myocardium / pathology*
  • Myocytes, Cardiac / metabolism*
  • Myocytes, Cardiac / pathology*
  • Okadaic Acid / pharmacology
  • Patch-Clamp Techniques
  • Protein Subunits / genetics
  • Protein Subunits / metabolism

Substances

  • Calcium Channels, L-Type
  • L-type calcium channel alpha(1C)
  • Protein Subunits
  • Okadaic Acid
  • 8-Bromo Cyclic Adenosine Monophosphate