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[阿吗灵及其治疗用衍生物N-丙基阿吗灵和二氯乙酰阿吗灵对豚鼠心房功能不应期和收缩性以及大鼠乌头碱心律失常的影响]

[Effect of ajmaline and its therapeutically used derivatives N-propylajmaline and di-monochloracetylajmaline on the functional refractory period and contractility of guinea pig atrium and aconitine arrhythmia in the rat].

作者信息

Raschack V M

出版信息

Arzneimittelforschung. 1975 Apr;25(4):639-41.

PMID:50847
Abstract
  1. In the isolated left atrium of the guinea pig ajmaline and di-monochloracetylajmaline (DCAA) show almost the same activity concerning prolongation of the functional refractory period. 2. In contrast to this N-propylajmaline (NPA) is much more effective than ajmaline. 3. NPA as compared to ajmaline and DCAA, however, shows a considerably smaller difference between the concentrations prolonging refractory period (I) and those decreasing contractility (II) in the guinea pig atrium (EC25). The quotient from I and II is 0.4 with NPA, 1.2 with ajmaline and 1.6 with DCAA. 4. Differences in efficacy similar to those observed in the guinea pig atrium are also found in experimental cardiac arrhythmias in the intact animal. NPA is much more effective than ajmaline regarding inhibition of extrasystoles, ventricular tachycardia and ventricular flutter due to aconitine infusion in the rat. In this experimental model DCAA shows slightly less activity than ajmaline; this difference is statistically significant.
摘要
  1. 在豚鼠离体左心房中,阿马林和二氯乙酰阿马林(DCAA)在延长功能不应期方面表现出几乎相同的活性。2. 与此相反,N-丙基阿马林(NPA)比阿马林更有效。3. 然而,与阿马林和DCAA相比,NPA在豚鼠心房中延长不应期的浓度(I)和降低收缩力的浓度(II)之间的差异要小得多(EC25)。NPA的I与II的商为0.4,阿马林为1.2,DCAA为1.6。4. 在完整动物的实验性心律失常中也发现了与豚鼠心房中观察到的类似的疗效差异。在大鼠中,由于乌头碱注入引起的室性早搏、室性心动过速和室性扑动,NPA在抑制方面比阿马林更有效。在这个实验模型中,DCAA的活性略低于阿马林;这种差异具有统计学意义。

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