Reduced effects of BAY K 8644 on L-type Ca2+ current in failing human cardiac myocytes are related to abnormal adrenergic regulation

Am J Physiol Heart Circ Physiol. 2008 May;294(5):H2257-67. doi: 10.1152/ajpheart.01335.2007. Epub 2008 Mar 21.

Abstract

Abnormal L-type Ca(2+) channel (LTCC, also named Cav1.2) density and regulation are important contributors to depressed contractility in failing hearts. The LTCC agonist BAY K 8644 (BAY K) has reduced inotropic effects on failing myocardium. We hypothesized that BAY K effects on the LTCC current (I(CaL)) in failing myocytes would be reduced because of increased basal activity. Since support of the failing heart with a left ventricular assist device (LVAD) improves contractility and adrenergic responses, we further hypothesized that BAY K effects on I(CaL) would be restored in LVAD-supported failing hearts. We tested our hypotheses in human ventricular myocytes (HVMs) isolated from nonfailing (NF), failing (F), and LVAD-supported failing hearts. We found that 1) BAY K had smaller effects on I(CaL) in F HVMs compared with NF HVMs; 2) BAY K had diminished effects on I(CaL) in NF HVM pretreated with isoproterenol (Iso) or dibutyryl cyclic AMP (DBcAMP); 3) BAY K effects on I(CaL) in F HVMs pretreated with acetylcholine (ACh) were normalized; 4) Iso had no effect on NF HVMs pretreated with BAY K; 5) BAY K effects on I(CaL) in LVAD HVMs were similar to those in NF HVMs; 6) BAY K effects were reduced in LVAD HVMs pretreated with Iso or DBcAMP; 7) Iso had no effect on I(CaL) in LVAD HVMs pretreated with BAY K. Collectively, these results suggest that the decreased BAY K effects on LTCC in F HVMs are caused by increased basal channel activity, which should contribute to abnormal contractility reserve.

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester / pharmacology*
  • Acetylcholine / pharmacology
  • Adrenergic beta-Agonists / pharmacology*
  • Bucladesine / pharmacology
  • Calcium Channel Agonists / pharmacology*
  • Calcium Channels, L-Type / drug effects*
  • Calcium Channels, L-Type / metabolism
  • Cardiotonic Agents / pharmacology*
  • Catecholamines / metabolism
  • Drug Resistance
  • Heart Failure / metabolism*
  • Heart Failure / physiopathology
  • Heart Failure / therapy
  • Heart Ventricles / drug effects
  • Heart Ventricles / metabolism
  • Heart-Assist Devices
  • Humans
  • Isoproterenol / pharmacology*
  • Membrane Potentials / drug effects
  • Myocardial Contraction / drug effects
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Phosphorylation

Substances

  • Adrenergic beta-Agonists
  • CACNA1C protein, human
  • Calcium Channel Agonists
  • Calcium Channels, L-Type
  • Cardiotonic Agents
  • Catecholamines
  • L-type calcium channel alpha(1C)
  • Bucladesine
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Isoproterenol
  • Acetylcholine