methaqualone

Small moleculeapproved

Approved

Jun 1, 1965

Methaqualone is a depressant that modulates the activity of the GABA receptors in the brain and nervous system. It promotes relaxation, sleepiness and sometimes a feeling of euphoria. It causes a drop in blood pressure and slows the pulse rate. These properties are the reason why it was initially thought to be a useful sedative and anxiolytic. Common side effects of Methaqualone include dizziness, nausea, vomiting, diarrhea, abdominal cramps, fatigue, itching, rashes, sweating, dry mouth, tingling sensation in arms and legs, seizures and its depressant effects include reduced heart rate and respiration. The drug became banned in many countries and was withdrawn from many markets in the early 1980s. — NCATS

Clinical trial activity

1 trials · 4 clinical orgs · 1 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Mar 1, 2005 (NCT00114855)

Timeline

1960s

Jun 1, 1965
Earliest FDA Approval

Indications

Approved for

Mechanism of action

GABA-A receptor; anion channelPOSITIVE ALLOSTERIC MODULATOR
GABA-A receptor; anion channel positive allosteric modulator
Methaqualone was demonstrated to be a positive allosteric modulator at human Alpha 1,2,3,5 Beta 2,3 Gamma 2S GABA A receptors (GABAARs) expressed in Xenopus oocytes, whereas it displayed highly diverse functionalities at the Alpha 4,6 Beta 1,2,3 Delta GABAAR subtypes, ranging from inactivity (Alpha4 Beta1 Delta), through negative (Alpha 6 Beta 1 Delta) or positive allosteric modulation (Alpha 4 Beta 2 Delta, Alpha 6 Beta 2,3 Delta), to superagonism (Alpha 4 Beta 3 Delta).
Proposed to act through the transmembrane beta(+)/alpha(-) subunit interface of the receptor, possibly targeting a site overlapping with that of the general anesthetic etomidate. It doesn't interact with the benzodiazepine, barbiturate, or neurosteroid binding sites.

Approval history

approvedJun 1, 1965

Chemistry & pharmacology

Loading structure…

SMILES

Cc1ccccc1-n1c(C)nc2ccccc2c1=O

Mol. weight: 250.3 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

Also known as

cateudyl
ci-705
ci-705
cn-38703
cn-38703
hypocol
hypocol
melsomin
metaqualon
methaqualon
methaqualone
methaqualone
methaqualone
methaqualone
methaqualone
methaqualone
methaqualone
methaqualone hcl
methaqualone hcl
methaqualone hydrochloride
methaqualone hydrochloride
methaqualoneinone
metolquizolone
optimil
optimil
parest
parest
quaalude
quaalude
quaalude
quaalude
quaalude
quaalude
quaalude
qz-2
qz-2
r-148
r-148
tr-495
tr-495
tuazole
tuazolone

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT00114855	N/A	Mar 1, 2005	Osaka University, Peking University, Pharmalogica, Wearnes Biotech and Medicals

Showing 1 of 1 trials

Page 1 / 1

Organizations

Research & Development (4)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Osaka University	Academic/Hospital	1	1	1	2005
Peking University	Academic/Hospital	1	0	1	2005
Pharmalogica	Academic/Hospital	1	0	1	2005
Wearnes Biotech and Medicals	For profit	1	0	1	2005

4 organizations

Page 1 / 1

Marketing (1)

Organization	Org type	Relationship	Date
Rhone Poulenc	For profit	NDA	—