Drug intelligence / Profile preview

methaqualone

Development stage
Discontinued
Lead developer
Wallace and Tiernan
Modality
Small Molecules
Administration
Oral, Inhalation, Intranasal
01

Overview

Methaqualone is a synthetic sedative-hypnotic drug belonging to the quinazolinone class. It was originally developed in India in the 1950s and patented in the United States by Wallace and Tiernan in 1962 for use as a treatment for insomnia and as a muscle relaxant[4][7]. Methaqualone acts primarily as a central nervous system depressant by modulating gamma-aminobutyric acid type A (GABA A) receptors. Specifically, it is a positive allosteric modulator at many GABA A receptor subtypes—enhancing inhibitory neurotransmission and producing sedation similar to barbiturates[1][2][6]. At some GABA A receptor subtypes it can act as a negative allosteric modulator. Its binding site on the GABA A receptor is distinct from those of benzodiazepines or barbiturates[2][8]. Methaqualone was widely prescribed under brand names such as Quaalude and Sopor but became notorious for its recreational abuse potential during the 1970s before being withdrawn from medical use due to high rates of addiction and overdose risk[3][6]. Today it has no accepted medical use in most countries.

Brand names
QuaaludeSoporMandrax
Other names
LudesMandrakeParestOptimilSomnafacToquilone Compositum
02

Targets

GABRR (GABA-A receptor subunit rho)

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