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血根碱:一种具有正性肌力作用的生物碱,可抑制心肌钠钾ATP酶。

Sanguinarine: a positive inotropic alkaloid which inhibits cardiac Na+,K+-ATPase.

作者信息

Seifen E, Adams R J, Riemer R K

出版信息

Eur J Pharmacol. 1979 Dec 20;60(4):373-7. doi: 10.1016/0014-2999(79)90245-0.

Abstract

In isolated, isometrically contracting left guinea pig atria, sanguinarine, a benzophenanthridine alkaloid from the papaveracea Sanguinaria canadensis, produced a concentration-dependent positive inotropic effect. Between 2.3 x 10(-6) M and 6.5 x 10(-5) M, sanguinarine increased contractility by 108% which was comparable to the maximal inotropic effect of ouabain. Within the same concentration range, sanguinarine caused inhibition of Na+,K+-ATPase isolated from guinea pig myocardium. 100% inhibition of Na+,K+,ATPase activity occurred at 1 x 10(-4) M sanguinarine. The I50 for enzyme inhibition and the ED50 for the inotropic action of sanguinarine were the same (6-6.5 x 10(-6) M) indicating that both effects may be causally related.

摘要

在分离的豚鼠左心房等长收缩实验中,血根碱(一种从罂粟科植物加拿大血根草中提取的苯并菲啶生物碱)产生了浓度依赖性正性肌力作用。在2.3×10⁻⁶ M至6.5×10⁻⁵ M之间,血根碱使收缩力增加了108%,这与哇巴因的最大正性肌力作用相当。在相同浓度范围内,血根碱可抑制从豚鼠心肌中分离出的Na⁺,K⁺-ATP酶。当血根碱浓度为1×10⁻⁴ M时,Na⁺,K⁺,ATP酶活性被100%抑制。血根碱对酶抑制的半数抑制浓度(I50)和对正性肌力作用的半数有效浓度(ED50)相同(6 - 6.5×10⁻⁶ M),表明这两种作用可能存在因果关系。

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