Key result
Protein kinase C activation with PDBu decreased ICa,L sensitivity to beta1-adrenergic receptor stimulation, promoting coupling of these receptors to Gi/o mediated inhibitory responses.
Population
Guinea pig ventricular myocytes
Comparison
Phorbol-12,13-dibutyrate treatment vs Inactive phorbol ester 4alpha-phorbol-12,13-didec…
Design
Preclinical
Authors
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Hypothesis-generating for PKC effects on myocyte signaling; should not change clinical practice pending human data.
Protein kinase C activation promotes the coupling of cardiac beta1-adrenergic and H2 histamine receptors to Gi/o mediated inhibitory responses in ventricular myocytes.
Belevych et al. (2003) studied this question. Phorbol-12,13-dibutyrate (PDBu) vs. Inactive phorbol ester 4alpha-phorbol-12,13-didecanoate was evaluated on L-type Ca2+ current (ICa,L) sensitivity to stimulation by submaximal beta1-AR activation. Protein kinase C activation with PDBu decreased ICa,L sensitivity to beta1-adrenergic receptor stimulation, promoting coupling of these receptors to Gi/o mediated inhibitory responses.
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