methaqualone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1739 72-44-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • quaalude
  • methaqualone
  • cateudyl
  • melsomin
  • metaqualon
  • methaqualon
  • methaqualoneinone
  • metolquizolone
  • tuazolone
  • tuazole
A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)
  • Molecular weight: 250.30
  • Formula: C16H14N2O
  • CLOGP: 2.75
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 32.67
  • ALOGS: -3.79
  • ROTB: 0

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.30 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 19.98 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1965 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05CM01 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Other hypnotics and sedatives
ATC N05CX02 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Hypnotics and sedatives in combination, excl. barbiturates
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
CHEBI has role CHEBI:35717 hypnotics
CHEBI has role CHEBI:51373 gamma-aminobutyric acid receptor agonist

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.56 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.41 SCIENTIFIC LITERATURE
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.52 SCIENTIFIC LITERATURE
GABA A receptor alpha-2/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.61 SCIENTIFIC LITERATURE
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.31 SCIENTIFIC LITERATURE
GABA A receptor alpha-4/beta-2/delta Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.17 SCIENTIFIC LITERATURE
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.56 SCIENTIFIC LITERATURE
GABA A receptor alpha-4/beta-3/delta Ion channel AGONIST EC50 3.91 SCIENTIFIC LITERATURE
GABA-A receptor alpha-6/beta-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.13 SCIENTIFIC LITERATURE
GABA-A receptor alpha-6/beta-2/delta Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.44 SCIENTIFIC LITERATURE
GABA-A receptor alpha-6/beta-3/delta Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.50 SCIENTIFIC LITERATURE

External reference:

IDSource
4027428 VUID
N0000176151 NUI
D00557 KEGG_DRUG
4027428 VANDF
C0025627 UMLSCUI
CHEBI:6821 CHEBI
CHEMBL282052 ChEMBL_ID
DB04833 DRUGBANK_ID
D008702 MESH_DESCRIPTOR_UI
6292 PUBCHEM_CID
966 INN_ID
7ZKH8MQW6T UNII
6823 RXNORM
001434 NDDF
71813009 SNOMEDCT_US

Pharmaceutical products:

None