Activation and modulation of recombinant glycine and GABA_A receptors by 4-halogenated analogues of propofol

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• 作者：Allison L Germann ; Daniel J Shin ; Brad D Manion ; Christopher J Edge ; Edward H Smith ; Nicholas P Franks ; Alex S Evers and Gustav Akk
• 刊名：British Journal of Pharmacology
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：173
• 期：21
• 页码：3110-3120
• 全文大小：892K
• ISSN：1476-5381

文摘

Glycine receptors are important players in pain perception and movement disorders and therefore important therapeutic targets. Glycine receptors can be modulated by the intravenous anaesthetic propofol (2,6-diisopropylphenol). However, the drug is more potent, by at least one order of magnitude, on GABA_A receptors. It has been proposed that halogenation of the propofol molecule generates compounds with selective enhancement of glycinergic modulatory properties.