EVIDENCE FOR THE INVOLVEMENT OF N-ACETYL-P-QUINONEIMINE IN ACETAMINOPHEN METABOLISM

EVIDENCE FOR THE INVOLVEMENT OF N-ACETYL-P-QUINONEIMINE IN ACETAMINOPHEN METABOLISM
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DOI:
10.1016/0006-2952(79)90123-0
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发表时间:
1979-01-01
影响因子:
5.8
通讯作者:
KISSINGER, PT
KISSINGER, PT
中科院分区:
医学2区
文献类型:
--
作者:
MINER, DJ;KISSINGER, PT

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N-乙酰基-对醌亚胺(NAPQI),一种假定的对乙酰氨基酚[镇痛剂]代谢的毒性中间体,在小鼠肝微粒体孵育的存在的证据报告。通过与在库仑流动反应器中由对乙酰氨基酚电化学产生的合成NAPQI进行比较,初步鉴定了中间体。NAPQI与一些亲核试剂的反应产物中除1种外,其他所有产物均在体外发现,且相对量相似。NAPQI中间体在生理pH和温度下中等稳定,其寿命取决于培养基的组分。
Evidence of the presence of N-acetyl-p-quinoneimine (NAPQI), a postulated toxic intermediate of acetaminophen [an analgesic] metabolism, in mouse liver microsomal incubations is reported. The intermediate was tentatively identified by comparison with synthetic NAPQI generated electrochemically from acetaminophen in a coulometric flow reactor. All but 1 of the reaction products of NAPQI with a number of nucleophiles were found in vitro as well, and in similar relative amounts. The NAPQI intermediate is moderately stable at physiological pH and temperature with a lifetime which is dependent on the components of the medium.