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| '''PWZ-029''' is a ] derivative drug with ] effects. 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>Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM. 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''. 2008 May 7;1208:150-9. PMID 18394590</ref> | '''PWZ-029''' is a ] derivative drug with ] effects. 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>Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM. 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''. 2008 May 7;1208:150-9. {{DOI|10.1016/j.brainres.2008.02.020}} PMID 18394590</ref> | ||
| ==See also== | ==See also== | ||
Revision as of 22:07, 3 January 2011
Pharmaceutical compound | |
| Identifiers | |
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IUPAC name
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| PubChem CID | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C14H14ClN3O2 |
| Molar mass | 291.732 g/mol g·mol |
| 3D model (JSmol) | |
SMILES
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PWZ-029 is a benzodiazepine derivative drug with nootropic effects. 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
- Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM. 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. 2008 May 7;1208:150-9. doi:10.1016/j.brainres.2008.02.020 PMID 18394590
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