Article
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).
Molecular pharmacology - 1 Aug 2015
Hammer Harriet, Bader Benjamin M, Ehnert Corina, Bundgaard Christoffer, Bunch Lennart, Hoestgaard-Jensen Kirsten, Schroeder Olaf H-U, Bastlund Jesper F, Gramowski-Voß Alexandra, Jensen Anders A
Abstract excerpt
In the present study, we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypnotic and recreational drug from the 1960s-1970s. Methaqualone was demonstrated to be a positive allosteric modulator at human α1,2,3,5β2,3γ2S GABAA receptors (GABAARs) expressed in Xenopus oocytes, whereas it displayed highly...
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