PPTQ

PPTQ
Clinical data
ATC code
  • none
Identifiers
  • 3-(4-methylphenyl)-2-phenylquinazolin-4-one
CAS Number
PubChem CID
Chemical and physical data
FormulaC21H16N2O
Molar mass312.372 g·mol−1
3D model (JSmol)
  • CC1=CC=C(C=C1)N2C(=NC3=CC=CC=C3C2=O)C4=CC=CC=C4
  • InChI=1S/C21H16N2O/c1-15-11-13-17(14-12-15)23-20(16-7-3-2-4-8-16)22-19-10-6-5-9-18(19)21(23)24/h2-14H,1H3
  • Key:QBGIEWLTLCNRED-UHFFFAOYSA-N

PPTQ, is an analogue of the sedative and hypnotic drug methaqualone first identified as a sedative drug in 2018. It is a derivative of methaqualone with the 2-methyl group replaced by a phenyl ring and the o-tolyl group replaced by p-tolyl. It acts as a potent GABAA receptor positive allosteric modulator, acting primarily at the α4β2δ subtype and to a lesser extent at the α1β2γ2S subtype, showing an overlap in its binding sites and modulatory activity with barbiturates and other sedatives such as propofol and etomidate, but acting in a way distinct from that of benzodiazepines. It has been sold as a designer drug and is reportedly up to 100x more potent than methaqualone as a sedative, and can similarly sometimes produce a paradoxical lowering of the seizure threshold. This makes methaqualone and its derivatives especially dangerous in overdose, as severely affected individuals can be simultaneously sedated to the point of unconsciousness but also experiencing convulsions, with administration of anticonvulsant drugs complicated by the need to avoid worsening sedation.

See also

References

  1. ↑ Madjroh N, Olander ER, Bundgaard C, Söderhielm PC, Jensen AA (January 2018). "Functional properties and mechanism of action of PPTQ, an allosteric agonist and low nanomolar positive allosteric modulator at GABAA receptors". Biochemical Pharmacology. 147: 153–169. doi:10.1016/j.bcp.2017.11.006. PMID 29155148.
  2. ↑ Chojnacka W, Teng J, Kim JJ, Jensen AA, Hibbs RE (19 June 2024). "Structural insights into GABAA receptor potentiation by Quaalude". Nature Communications. 15 (1) 5244. doi:10.1038/s41467-024-49471-y. PMC 11187190. PMID 38898000.
  3. ↑ Wachełko O, Tusiewicz K, Zawadzki M, Szpot P (June 2026). "Reinventing quaaludes: a comprehensive review of designer methaqualone analogs". Forensic Toxicology. doi:10.1007/s11419-026-00773-4. PMID 42289025.