钱元恕, 全钰珠. 吡喹酮及其对映异构体对离体大鼠心房肌生理特性的影响J. 药学学报, 1988, 23(11): 812-816.
引用本文: 钱元恕, 全钰珠. 吡喹酮及其对映异构体对离体大鼠心房肌生理特性的影响J. 药学学报, 1988, 23(11): 812-816.
YS Qian, YZ Quan. EFFECTS OF PRAZIQUANTEL AND ITS ENANTIOMERS ON THE PHYSIOLOGICAL PROPERTIES OF ISOLATED RAT ATRIAJ. Acta Pharmaceutica Sinica, 1988, 23(11): 812-816.
Citation: YS Qian, YZ Quan. EFFECTS OF PRAZIQUANTEL AND ITS ENANTIOMERS ON THE PHYSIOLOGICAL PROPERTIES OF ISOLATED RAT ATRIAJ. Acta Pharmaceutica Sinica, 1988, 23(11): 812-816.

吡喹酮及其对映异构体对离体大鼠心房肌生理特性的影响

EFFECTS OF PRAZIQUANTEL AND ITS ENANTIOMERS ON THE PHYSIOLOGICAL PROPERTIES OF ISOLATED RAT ATRIA

  • 摘要: 吡喹酮(praziquantel,PQT)对心肌生理特性的影响有立体选择性。(-)-PQT对离体大鼠左心房的正性肌力作用的效能和强度均比(+)-PQT和(±)-PQT小。用维拉帕米可明显减弱PQT及其对映异构体的正性肌力作用。在浓度为100μmol/1时,PQT及其对映异构体对离体大鼠右心房均有负性频率作用,而当30μmol/1时仅(+)-PQT对频率有明显影响。它们尚可诱发右心房心律失常,其发生率以(+)-PQT最高,(-)-PQT最低,(±)-PQT居中。(+)-和(±)-PQT可明显缩短左房不应期。(+)-PQT还可明显降低左房自律性,而(-)-PQT对不应期,自律性均无影响。

     

    Abstract: The stereoselectivity of the arrythmic effect of praziquantel (PQT)which contained a chiral carbon at position 11b of its moiety was reported in the previous study. In this study the effects of enantiomers of PQT on the physiological properties of isolated rat atria were shown to be different. ED50 of (±)-,(+)-and (-)-PQT calculated from the log dose-positive inotropic effect curve in left atria were 14.8, 16.6 and 48.0 μmol/L, respectively. The Emax of (-)-PQT was 49± 11% increase in contractile force, whereas that of (+)- and (±)- PQT were 85± (SD)15% and 79±(SD)4%, respectively. Verapamil in a very low concentration of 0.1μmol/L or 0.5 μmol/L antagonized the positive inotropic effects of PQT and its enantiomers very markedly. In low concentration(30μmol/L) only (+)-PQT and (±) PQT exhibited bradycardiac effect while in higher concentration (100 μmol/L) all three drugs exerted the same effect. These drugs could also induce arrythmias in right atria, but the frequency of arrythmias occurred in the right atria treated with (+)-PQT was much higher than that treated with (-)-PQT. (+)-PQT shortened the refractory period and decreased the automaticity of the left atria but (-)-PQT did not exert any effect on the refractory period and automaticity.

     

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