...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Amantadine acetylation may be effected by acetyltransferases other than NAT1 or NAT2.
【24h】

Amantadine acetylation may be effected by acetyltransferases other than NAT1 or NAT2.

机译：金刚烷胺的乙酰化可能受除NAT1或NAT2以外的乙酰转移酶的影响。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Amantadine is a drug with a primary amino group, and consequently a likely candidate for metabolism by acetylation. This study assessed the possibility that a person's polymorphic (NAT2) acetylator phenotype could be used to predict the extent of amantadine acetylation. Thirty-eight normal, healthy volunteers were NAT2 acetylator phenotyped with sulfapyridine. Of the six fastest (75-86%) and six slowest (34-40%) sulfapyridine acetylators, two and three, respectively, had acetylamantadine present (18-338 microg) in the 8-h urine collection. There was no correlation between NAT2 acetylator phenotype and amantadine acetylation (p<0.5), and no difference in the total urine amantadine excreted over 8 h between acetylators and nonacetylators (28.3+/-9.7 vs. 30.4+/-9.6 mg, respectively, mean +/- SD). Acetylamantadine represented 0.1-1.5% (median 0.5%) of urinary drug content over 8 h. Our data confirm that amantadine is acetylated in humans and demonstrate for the first time that the extent is not correlated with NAT2 acetylator phenotype. Parallel in vitro enzyme studies indicate the possibility that neither NATI nor NAT2 is responsible for acetylation of amantadine.
机译：金刚烷胺是具有伯氨基的药物，因此可能是通过乙酰化进行代谢的候选药物。这项研究评估了人的多态性（NAT2）乙酰化酶表型可用于预测金刚烷胺乙酰化程度的可能性。 38名正常，健康的志愿者是用磺胺吡啶定型的NAT2乙酰化酶。在六个最快的（75-86％）和六个最慢的（34-40％）的磺胺吡啶乙酰化剂中，在8小时的尿液收集中分别有两个和三个有乙酰金刚烷胺（18-338微克）。 NAT2乙酰化酶表型和金刚烷胺乙酰化之间没有相关性（p <0.5），乙酰化剂和非乙酰化剂在8小时内排泄的总尿金刚烷胺没有差异（分别为28.3 +/- 9.7和30.4 +/- 9.6 mg，平均值+/- SD）。在8小时内，乙酰胺基金刚烷胺占尿药含量的0.1-1.5％（中位数0.5％）。我们的数据证实金刚烷胺在人体内被乙酰化，并首次证明其程度与NAT2乙酰化剂表型无关。并行的体外酶研究表明，NATI和NAT2都不负责金刚烷胺的乙酰化。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号