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CHENG Yu-si, DAI De-zai, JI Hui, DAI Yin. Mechanism of endothelin receptor antagonist CPU0213 and calcium antagonist CPU86017 ameliorated rats′ heart failure induced by isoproterenol[J]. Journal of China Pharmaceutical University, 2011, 42(1): 58-63.
Citation: CHENG Yu-si, DAI De-zai, JI Hui, DAI Yin. Mechanism of endothelin receptor antagonist CPU0213 and calcium antagonist CPU86017 ameliorated rats′ heart failure induced by isoproterenol[J]. Journal of China Pharmaceutical University, 2011, 42(1): 58-63.

Mechanism of endothelin receptor antagonist CPU0213 and calcium antagonist CPU86017 ameliorated rats′ heart failure induced by isoproterenol

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  • The purpose of this experiment was to verify whether endothelin receptor antagonist CPU0213 and calcium antagonist CPU86017 improved isoproterenol (ISO)-induced heart failure in rats by inhibiting p66Shc and PKCε .40 SD male rats were randomly divided into 5 groups.Except for the normal group,the other groups were given isoproterenol for 10 d (1mg/kg,sc).Three treatment groups (sc,mg/kg,from day 10-11) included: aminoguanidine group 30 and CPU0213 group 30 and CPU86017 group 4.It was found that mRNA or the protein expressions of endothelin receptor A (ETA),iNOS,p66Shc,PKCε,OBRb,NADPH oxidase p67 phox and leptin increased in ISO group.After drug treatment ,the above abnormal indicators were mitigated and even reversed.Hence,it suggested that CPU0213 and CPU86017 improved the ISO- induced heart failure by inhibiting the endothelin receptor and oxidative stress and down-regulating the expressions of p66Shc and PKCε.
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