Ariëns E J
Eur J Clin Pharmacol. 1984;26(6):663-8. doi: 10.1007/BF00541922.
The significance of stereochemistry in therapeutic action is outlined and elucidated. Often only one isomer is therapeutically active, but this does not mean that the other is really inactive. It may very well contribute to the side-effects. The therapeutically non-active isomer in a racemate should be regarded as an impurity (50% or more). It is emphasized how in clinical pharmacology, and particularly in pharmacokinetics, neglect of stereoselectivity in action leads to the performance of expensive "highly sophisticated scientific nonsense". This also holds true in the development and marketing of new drugs as exemplified by various "pseudo-hybrid" drugs now reaching the clinic.
立体化学在治疗作用中的重要性已被概述和阐明。通常只有一种异构体具有治疗活性,但这并不意味着另一种异构体真的无活性。它很可能会导致副作用。外消旋体中无治疗活性的异构体应被视为杂质(50%或更多)。文中强调了在临床药理学,尤其是药代动力学中,作用中对立体选择性的忽视如何导致进行昂贵的“高度复杂的科学无意义行为”。这在新药的研发和上市中也同样适用,各种现已进入临床的“伪杂交”药物就是例证。