Using Deuterium in Drug Discovery: Leaving the Label in the Drug
Using Deuterium in Drug Discovery: Leaving the Label in the Drug
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DOI：
10.1021/jm4007998
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发表时间：
2014-05-08
影响因子：
7.3
通讯作者：
Gant, Thomas G.
中科院分区：
文献类型：
--
作者：
Gant, Thomas G.
氘是氢的稳定同位素，它在机理、光谱和示踪研究中的应用为药物化学家所熟知。事实上，利用氘的众所周知的应用存在于药物发现和开发的每个子学科中。最近强调将氘掺入活性药物成分是由于对氘动力学同位素效应对原料药的安全性和处置的实质性益处的潜力进行了调查。这种观点追溯了作者在恢复和扩大这种潜在效用方面的经验，这种最简单的同位素的发现者在几十年前首次提出。
Deuterium, the stable isotope of hydrogen, is known to medicinal chemists for its utility in mechanistic, spectroscopic, and tracer studies. In fact, well-known applications utilizing deuterium exist within every subdiscipline in pharmaceutical discovery and development. Recent emphasis on incorporation of deuterium into the active pharmaceutical ingredient has come about as a result of inquiries into the potential for substantial benefits of the deuterium kinetic isotope effect on the safety and disposition of the drug substance. This Perspective traces the author's experience in reviving and expanding this potential utility, first suggested many decades prior by the discoverer of this, the simplest of all isotopes.