Bufadienolidesと数種の強心薬のモルモット心臓に対する作用

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Effects of bufadienolides such as bufalin (BF) and cinobufagin (CB), the main components of Senso (Ch'an Su) , on myocardial Na+, K+-ATPase activity, the cardiotonic activity in vivo and the action potential of isolated guinea pig papillary muscle cells were compared with those of other cardiotonic drugs. 1) The rank order of potency for inhibition of myocardial Na+, K+-ATPase activity was BF >digoxin (DG) > digitoxin (DT) > telocinobufagin > gamabufotalin > cinobufotalin > CB > g-strophanthin (GS) > digitoxigenin (DTG) > resibufogenin (RB) when compared at the 50% inhibitory concen tration. 2) In isolated papillary muscle cells, CB shortened the action potential duration (APD) dose dependently. The order of potency for shortening of APD was GS > CB > DTG>>DT. 3) In open-chest guinea pigs, intraduodenal administration of BF or CB increased the myocardial contractile force (MCF), but did not affect the heart rate. The order of potency for increase in MCF was as follows : methyldigoxin, proscillaridin > BF > CB >DG> Senso>>DT, DTG, RB. These results indicate that CB has a shortening effect on APD and an inhibitory effect on Nat, K+-ATPase activity along with its car diotonic effect, like GS.
社団法人日本薬理学会の論文