INVOLVEMENT OF CYP2D6, CYP3A4, AND OTHER CYTOCHROME-P-450 ISOZYMES IN N-DEALKYLATION REACTIONS

被引：80

作者：

COUTTS, RT ^{[1
]}

SU, P ^{[1
]}

BAKER, GB ^{[1
]}

机构：

[1] UNIV ALBERTA,DEPT PSYCHIAT,EDMONTON,AB,CANADA

来源：

JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS | 1994年 / 31卷 / 04期

关键词：

METABOLIC N-DEALKYLATION; CYTOCHROME P-450 ISOZYMES; CYP2D6; CYP3A ISOZYMES; DRUG METABOLISM;

D O I：

10.1016/1056-8719(94)90001-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Metabolic N-dealkylation is a commonly observed biotransformation with tertiary and secondary amine drugs and related N-alkylated amides, but surprisingly little is known about the cytochrome P-450 isozymes involved in these dealkylation reactions. In this review, evidence is provided that supports the involvement of various P-450 isozymes, but especially CYP3A4 and other isozymes of the CYP3A subfamily. Although CYP2D6 is generally not considered to be capable of catalyzing the N-dealkylation of basic drugs, some examples of the involvement of this important isozyme in N-dealkylation reactions are identified. Procedures used to identify individual P-450 isozymes involved in N-dealkylation reactions are discussed.

引用

收藏

页码：177 / 186

页数：10

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