Original Articles

Effects of changrolin and pyracrine phosphate on ATPase of rabbit heart sarcolemma

En-hong Chen, Zeng-hong Tu, Hui-hua Yang, Wei-wei Wu


Changrolin, 4-{3’,5’-bis [(N-pyrrolidinyl) methyl]-4’-hydroxy-anilino} quinazoline, was synthesized in our institute for treatment of arrhythmia. When the quinazoline ring of changrolin was substituted by an acridine ring, the compound was named pyracrine phosphate.
The rabbit heart sarcolemma was prepared according to the method of McNa-mara(5), except that the left ventricle was homogenized by a glass homogenizer and, in the last step, the membrane was extracted with 2 M LiBr. The inhibitory effects of changrolin and quinidine (1 mM) on the Na+, K+-ATPase activity were 24% and 50%, respectively.
The inhibitory effects of pyracrine phosphate and mepacrine on Na+, K+-ATPase were more potent. The inhibitory effect of pyracrine phosphate was similar to that of ouabain.
The effects of changrolin and pyracrine phosphate on Ca2+-ATPase activity were not significant at 0.5 and 1 mM.

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