PWZ-029

Chemical compound
PWZ-029
Identifiers
  • 8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
PubChem CID
  • 9971547
ChemSpider
  • 8147139 ☒N
ChEMBL
  • ChEMBL45346 ☒N
Chemical and physical data
FormulaC14H14ClN3O2
Molar mass291.74 g·mol−1
3D model (JSmol)
  • Interactive image
  • ClC1=CC=C2C(C(N(CC3=C(COC)N=CN32)C)=O)=C1
InChI
  • InChI=1S/C14H14ClN3O2/c1-17-6-13-11(7-20-2)16-8-18(13)12-4-3-9(15)5-10(12)14(17)19/h3-5,8H,6-7H2,1-2H3 ☒N
  • Key:FXIDXTIMKAEBGY-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

PWZ-029 is a benzodiazepine derivative drug with nootropic effects developed by WiSys,[1] It acts as a subtype-selective, mixed agonist-inverse agonist at the benzodiazepine binding site on the GABAA receptor, acting as a partial inverse agonist at the α5 subtype and a weak partial agonist at the α3 subtype. This gives it a mixed pharmacological profile, producing at low doses memory-enhancing effects but with no convulsant or anxiogenic effects or muscle weakness, although at higher doses it produces some sedative effects.[2]

See also

  • GABAA receptor negative allosteric modulator
  • GABAA receptor § Ligands
  • GL-II-73

References

  1. ^ US Patent application US2006/258643 A1
  2. ^ Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM (May 2008). "PWZ-029, a compound with moderate inverse agonist functional selectivity at GABA(A) receptors containing alpha5 subunits, improves passive, but not active, avoidance learning in rats". Brain Research. 1208: 150–9. doi:10.1016/j.brainres.2008.02.020. PMC 2577822. PMID 18394590.
  • v
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GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAATooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators
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1,4-Benzodiazepines
1,5-Benzodiazepines
2,3-Benzodiazepines*
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Thienotriazolodiazepines
Thienobenzodiazepines*
Pyridodiazepines
Pyridotriazolodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Pyrrolobenzodiazepines*
Benzodiazepine prodrugs
* atypical activity profile (not GABAA receptor ligands)


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