Stress-up-regulated myocardial endothelin receptors are suppressed by chlorobenzyltetrahydroberberine CPU86017 and its RS chiral isomer

Aim ：To investigate the changes of endothelin(ET)receptors by isoproterenol in myocardial cells，and the invervention effects of CPU86017 and its RS isomer. Methods ：Primary cultures of neonatal rat cardiomyocytes were prepared，and isoproterenol was added to each group for modeling，followed by drug interventions with propranolol，CPU86017 and RS chiral isomer respectively. Results ：The expressions of ET_A and ET_B were increased by isoproterenol，in which the level of ET_B was higher than ET_A .This phenomenon was adjusted to different degrees by using propranolol，CPU86017 and RS chiral isomer in a dosage-relevant manner.The infervention effect of RS isomer was better than that of CPU86017 at the high dosage(10 μmol/L). Conclusion ：The cardiovascular effects of CPU86017 and RS chiral isomer could be correlative to the inhibition of the over-expressions of ET_A and ET_B.