Grimmer I, Moller R, Gross J, Gmyrek D, Klinger W
Biol Neonate. 1981;40(5-6):218-23. doi: 10.1159/000241495.
The aim of this paper is to report on the influence of phenobarbital, the combination of phenobarbital/nikethamide, the racemate and (+) isomer of methylphenobarbital on the activity of bilirubin UDP-glucuronyltransferase and the concentration of intrahepatic Y and Z protein in rats. The activity of bilirubin DP-glucuronyltransferase increased after the treatment in all groups. Pretreatment with phenobarbital/nikethamide resulted in the highest enzyme activity, using wet weight as reference. (+) Methylphenobarbital isomer as well as the racemate showed effects similar to those of phenobarbital. The concentration of hepatic Y acceptor protein increased in all pretreated groups by about 30%. The drugs did not increase the concentration of Z protein. The (+) isomer of methylphenobarbital seems better suited as an inductive drug in the prophylaxis of hyperbilirubinemia and in the treatment of nonconjugated hyperbilirubinemia than phenobarbital or phenobarbital/nikethamide since it has no sedative effect.
本文旨在报道苯巴比妥、苯巴比妥/尼可刹米组合、甲基苯巴比妥外消旋体及(+)异构体对大鼠胆红素UDP-葡萄糖醛酸基转移酶活性及肝内Y蛋白和Z蛋白浓度的影响。所有组在处理后胆红素DP-葡萄糖醛酸基转移酶活性均升高。以湿重为参照,苯巴比妥/尼可刹米预处理导致酶活性最高。(+)甲基苯巴比妥异构体以及外消旋体显示出与苯巴比妥相似的效果。所有预处理组肝Y受体蛋白浓度增加约30%。这些药物未增加Z蛋白浓度。甲基苯巴比妥(+)异构体似乎比苯巴比妥或苯巴比妥/尼可刹米更适合作为预防高胆红素血症及治疗非结合型高胆红素血症的诱导药物,因为它没有镇静作用。