Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee 37232, United States.
Department of Anesthesiology, Vanderbilt University Medical Center, Nashville, Tennessee 37232, United States.
ACS Chem Neurosci. 2023 Feb 1;14(3):340-350. doi: 10.1021/acschemneuro.2c00697. Epub 2023 Jan 18.
Commonly known as "Quaaludes," methaqualone () is a sedative-hypnotic medication, with effects resembling barbiturates and other downers, that exerts its effects through modulation of γ-aminobutyric acid type A receptors (GABAR). Following the discovery of the sedative and euphoric effects of methaqualone (), it was quickly adopted by pharmaceutical companies and promoted by clinicians around the world as a "safe" sleeping pill option, and for a period it was available over the counter. The popularity of methaqualone () soared worldwide, and many people began to use it recreationally for its sedative-hypnotic-like psychoactive effects. Not long after its introduction, many individuals began to misuse the drug leading to overdoses and drug dependence which brought to light methaqualone's () addictive nature. In this review, the background, synthesis, pharmacology, metabolism, and pharmacokinetics of methaqualone () will be covered along with its discovery, history, and the derivatives that are currently available around the world through manufacture in clandestine laboratories.
通常被称为“Quaaludes”的甲喹酮（methaqualone）是一种镇静催眠药物，其作用类似于巴比妥类药物和其他镇静剂，通过调节γ-氨基丁酸 A 型受体（GABAR）发挥作用。甲喹酮（methaqualone）镇静和欣快作用被发现后，它很快被制药公司采用，并被世界各地的临床医生推广为一种“安全”的安眠药选择，并且在一段时间内可以在柜台上买到。甲喹酮（methaqualone）在全球范围内广受欢迎，许多人开始将其用于娱乐目的，因为它具有镇静催眠样的精神活性作用。在其推出后不久，许多人开始滥用该药物，导致过量用药和药物依赖，这凸显了甲喹酮（methaqualone）的成瘾性。在这篇综述中，将介绍甲喹酮（methaqualone）的背景、合成、药理学、代谢和药代动力学，以及它的发现、历史和目前通过秘密实验室制造在全球范围内可获得的衍生物。
