Misplaced Pages

PWZ-029: Difference between revisions

Article snapshot taken from Wikipedia with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
Browse history interactively← Previous editNext edit →Content deleted Content addedVisualWikitext
Revision as of 22:16, 28 July 2020 editBsherrAWBBOT (talk | contribs)Bots11,152 edits orphaning per Misplaced Pages:Templates for discussion/Log/2020 July 17#Template:Nootropics, plus general fixesTag: AWB← Previous edit Revision as of 06:37, 4 December 2020 edit undoMonkbot (talk | contribs)Bots3,695,952 editsm Task 18 (cosmetic): eval 1 template: del empty params (1×);Tag: AWBNext edit →
Line 46: Line 46:
}} }}


'''PWZ-029''' is a ] derivative drug with ] effects developed by WiSys,<ref>US Patent application US2006/258643 A1</ref> It acts as a subtype-selective, mixed agonist-inverse agonist at the ] binding site on the ] ], acting as a partial ] at the ] and a weak ] at the ]. This gives it a mixed pharmacological profile, producing at low doses memory-enhancing effects but with no ] or ] effects or muscle weakness, although at higher doses it produces some sedative effects.<ref name="pmid18394590">{{cite journal | vauthors = Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM | title = 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 | journal = Brain Research | volume = 1208 | issue = | pages = 150–9 | date = May 2008 | pmid = 18394590 | pmc = 2577822 | doi = 10.1016/j.brainres.2008.02.020 }}</ref> '''PWZ-029''' is a ] derivative drug with ] effects developed by WiSys,<ref>US Patent application US2006/258643 A1</ref> It acts as a subtype-selective, mixed agonist-inverse agonist at the ] binding site on the ] ], acting as a partial ] at the ] and a weak ] at the ]. This gives it a mixed pharmacological profile, producing at low doses memory-enhancing effects but with no ] or ] effects or muscle weakness, although at higher doses it produces some sedative effects.<ref name="pmid18394590">{{cite journal | vauthors = Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM | title = 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 | journal = Brain Research | volume = 1208 | pages = 150–9 | date = May 2008 | pmid = 18394590 | pmc = 2577822 | doi = 10.1016/j.brainres.2008.02.020 }}</ref>


==See also== ==See also==

Revision as of 06:37, 4 December 2020

Pharmaceutical compound
PWZ-029
Identifiers
IUPAC name
  • 8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazobenzodiazepin-6-one
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H14ClN3O2
Molar mass291.74 g·mol
3D model (JSmol)
SMILES
  • 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
  • Key:FXIDXTIMKAEBGY-UHFFFAOYSA-N
  (what is this?)  (verify)

PWZ-029 is a benzodiazepine derivative drug with nootropic effects developed by WiSys, 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.

See also

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.
GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip 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
Benzodiazepines
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)


Stub icon

This drug article relating to the nervous system is a stub. You can help Misplaced Pages by expanding it.

Categories: