艾司佐匹克隆的药物化学

Esopiclone of Medicinal Chemistry

失眠症的药物治疗已经历了巴比妥类、苯二氮卓类(BZ)和非BZ短效药物3个阶段。佐匹克隆属于非苯二氮卓类药物。艾司佐匹克隆是佐匹克隆的右旋异构体,是环吡咯酮类镇静催眠药,通过作用于苯二氮卓类(ω1型受体)-GABAA受体复合物特异的结合位点而发挥改善睡眠的作用。它在药效与药动以及临床治疗等方面都具有与苯二氮卓类药物不同的特点。本文讨论了艾司佐匹克隆的结构、理化性质、发现过程、构效关系、药理药动特点。

Insomnia drug therapy has a barbiturate,benzodiazepine class（BZ）and the three-stage non-BZ short-acting drugs.Zopiclone belongs to the nonbenzodiazepine class.Eszopiclone the（S）-enantiomer of the chiral hypnotic drug zopiclone,belongs to the cyclopyrrolone class of hypnotic drugs and acts as agonist at the type A γ-aminobutyric acid（GABA）receptor（ω1subtype）to improve the sleep quality.It has different characteristics in pharmacokinetics、pharmacodynamics and clinical treatment with benzodiazepine.This paper discusses the structure, physical and chemical properties, the discovery process, the structure - activity relationship, and pharmacological and pharmacokinetics characteristics of Eszopiclone.