Department of Anesthesia, Stanford School of Medicine, 300 Pasteur Dr., Stanford, CA 94305-5117, USA.
Anesth Analg. 2012 Aug;115(2):270-3. doi: 10.1213/ANE.0b013e31824a0b3c. Epub 2012 Feb 17.
The accompanying articles in this issue of the journal's special collection describe attempts to improve on the dynamics of distribution and reduce side effects of analogs of etomidate and benzodiazepines. Both classes of drugs have their principal sites of action on γ-aminobutyric acid type A receptors, although at very different binding sites and by different mechanisms of action. Herein, we review the structure of γ-aminobutyric acid type A receptors and describe the location of the 2 likely binding sites. In addition, we describe how these drugs can interact with the nervous system at a systems level. We leave it to other reviewers to discuss whether these new drugs offer true clinical improvements.
本期杂志特刊中的相关文章描述了旨在改善依托咪酯和苯二氮䓬类药物类似物的分布动力学并减少其副作用的尝试。这两类药物的主要作用部位均在γ-氨基丁酸 A 型受体上,尽管它们的结合部位和作用机制非常不同。本文综述了γ-氨基丁酸 A 型受体的结构,并描述了 2 个可能的结合部位的位置。此外,我们还描述了这些药物如何在系统水平上与神经系统相互作用。至于这些新药是否真正提供了临床改善,我们将留给其他评论者来讨论。