PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-? (PPAR-?) AGONIST INDUCE SENSITIZATION ?1 ADRENERGIC RECEPTOR VIA REGULATION EXTRACELLULAR SIGNAL-REGULATED KINASE 1/2 (ERK 1/2) AND G PROTEIN-COUPLED RECEPTOR KINASE-2 (GRK-2) IN CULTURE CARDIOMYOCYTE
Rachmat Hidayat* and Patricia Wulandari
ABSTRACT
The present study evaluated effect of pioglitazone (PPAR γ agonist) to sensitize β1-adrenergic receptor in culture cardiomyocyte. Up-regulated GRK2 and down-regulated of β1-adrenergic receptor in the heart underlies the diminished contractile responsiveness of the heart to positive inotropes. The result of study showed that potention of pioglitazone to increase or sensitize β1-adrenergic receptor via increase ERK1/2 and decrease GRK-2. The potention pioglitazone to increase concentration of β1-adrenergic receptor not only based on dose-dependent of pioglitazone but also influenced by concentration of norepinephrine.
Keywords: Pioglitazon – PPAR ? Agonist – ?1 adrenergic – GRK2 – ERK1/2.
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