Iwahashi K, Matsuo Y, Tsuneoka Y, Ichikawa Y, Hosokawa K, Suwaki H
Department of Psychiatry, Kagawa Medical School, Japan.
Arch Toxicol. 1993;67(7):514-6. doi: 10.1007/BF01969924.
The effects of histamine and 1-methyl-6,7-dihydroxy-1,2,3,4- tetrahydroisoquinoline(salsolinol) on debrisoquine 4-monooxygenation, which is catalyzed by cytochrome P-450db 1 (CYP2D1) in rat liver microsomes, were studied. Both histamine and salsolinol competitively inhibited the activity of debrisoquine 4-monooxygenase (Ki = 0.31 and 0.43 mM, respectively). These data demonstrate that histamine and salsolinol bind to the active site of CYP2D1, i.e. histamine and salsolinol have structures (molecular shape) corresponding to the active site of CYP2D1.
研究了组胺和1-甲基-6,7-二羟基-1,2,3,4-四氢异喹啉（salsolinol）对大鼠肝微粒体中由细胞色素P-450db 1（CYP2D1）催化的异喹胍4-单加氧作用的影响。组胺和salsolinol均竞争性抑制异喹胍4-单加氧酶的活性（Ki分别为0.31和0.43 mM）。这些数据表明，组胺和salsolinol与CYP2D1的活性位点结合，即组胺和salsolinol具有与CYP2D1活性位点相对应的结构（分子形状）。
