Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter.
Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter.
复制标题
4-羟基安替比林及其4-O-硫酸盐对安替比林生物分布促进剂的影响。
DOI：
10.1248/bpb.24.529
复制
发表时间：
2001
影响因子：
2
通讯作者：
T. Nakayama
中科院分区：
文献类型：
--
作者：
Y. Ohkawa;M. Matsumura;Y. Kurosaki;M. Kurumi;K. Sasaki;T. Nakayama
研究了安替比林主要代谢物4-羟基安替比林（4-OH）及其4- o -硫酸盐（4-S）对安替比林大鼠药动学的影响。在稳态4-OH浓度下，静脉给药安替比林的血浆消除明显减慢，而在稳态4-S浓度下则没有。同时使用4-OH可显著提高安替比林稳态浓度下的脑组织和心脏组织血药浓度比（Kp），而类似使用4-S则无影响。同时使用4-OH导致安替比林血脑屏障（BBB）通透性增强，认为与安替比林脑内Kp值升高有关。这些结果表明4-OH可以作为生物分布促进剂。
The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine, and its 4-O-sulfate (4-S) on the pharmacokinetics of antipyrine were investigated in rats. Plasma elimination of intravenously administered antipyrine was significantly decelerated under a steady-state concentration of 4-OH but not under that of 4-S. Tissue-to-plasma concentration ratio (Kp) of antipyrine under its steady-state concentration was significantly increased in the brain and heart by the concomitant use of 4-OH, while similar use of 4-S had no effect. The enhancement of the blood-brain barrier (BBB) permeability of antipyrine caused by the concomitant use of 4-OH was believed to be concerned with the increase of the Kp value of antipyrine in the brain. These results suggested that 4-OH could be used as a biodistribution promoter.
DOI：
10.1248/bpb1978.4.879
发表时间：
1981-01-01
期刊：
JOURNAL OF PHARMACOBIO-DYNAMICS
影响因子：
--
作者：
YAMAOKA, K;TANIGAWARA, Y;UNO, T
通讯作者：
UNO, T