METABOLISM AND PHARMACOKINETICS OF CINOBUFAGIN
METABOLISM AND PHARMACOKINETICS OF CINOBUFAGIN
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DOI：
10.3109/00498258709167411
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发表时间：
1987-10-01
期刊：
影响因子：
1.8
通讯作者：
KAWAKAMI, M
中科院分区：
文献类型：
--
作者：
TOMA, S;MORISHITA, S;KAWAKAMI, M
1. 研究了大鼠静脉注射促心药Senso的主要成分蟾毒素的代谢命运。在大鼠血清中检测到两种代谢物，经核磁共振和质谱分析，分别为去乙酰化蟾毒蛋白(I)和3-乙酰化蟾毒蛋白（II）。I和II对豚鼠心脏Na+/K+- atp酶的抑制作用均小于蟾毒球蛋白。3. 大鼠、猫和狗在静脉注射和/或口服牛瘟毒蛋白后，采用高效液相质谱法测定血清或血浆中牛瘟毒蛋白、I和II的水平。静脉给药后，大鼠血清中出现了蟾毒蛋白I和II，但在狗和猫血浆中只有不变的蟾毒蛋白存在。口服给药后，大鼠血清中仅检测到II，而猫和狗血清中均未检测到蟾毒球蛋白及其代谢产物（I和II）。
1. The metabolic fate of cinobufagin, a major component of the cardiotonic Senso, has been studied after i.v. administration to rats. Two metabolites were detected in rat serum and shown by n.m.r. and mass spectroscopy to be desacetylcinobufagin (I) and 3-epidesacetylcinobufagin (II). 2. Inhibitory activities of I and II on guinea-pig heart Na+/K+-ATPase were less than that of cinobufagin. 3. Serum or plasma levels of cinobufagin, I and II in rats, cats and dogs were determined by h.p.l.c. after i.v. and/or oral administration of cinobufagin. After i.v. administration, cinobufagin, I and II appeared in rat serum, but in dog and cat plasma only unchanged cinobufagin was present. After oral administration, only II was detected in rat serum, but neither cinobufagin nor either of its metabolites (I and II) were found in cat and dog serum.