A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).

@article{Hammer2015AMG,
  title={A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).},
  author={Harriet Hammer and Benjamin M. Bader and Corina Ehnert and Christoffer Bundgaard and Lennart Bunch and Kirsten Hoestgaard-Jensen and Olaf Jens Schr{\"o}der and Jesper Frank Bastlund and Alexandra Gramowski-Voss and Anders A Jensen},
  journal={Molecular pharmacology},
  year={2015},
  volume={88 2},
  pages={
          401-20
        }
}
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 diverse functionalities at the α4,6β1,2,3δ GABAAR subtypes, ranging from inactivity… CONTINUE READING
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