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{{short description|Chemical compound}}
{{Drugbox {{Drugbox
| Verifiedfields = changed
| Watchedfields = changed | Watchedfields = changed
| verifiedrevid = 424715425 | verifiedrevid = 424715425
| IUPAC_name = 8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazobenzodiazepin-6-one | IUPAC_name = 8-chloro-3-(methoxymethyl)-5-methyl-4''H''-imidazobenzodiazepin-6-one
| image = PWZ-029_structure.png | image = PWZ-029.svg


<!--Clinical data--> <!--Clinical data-->
| tradename = | tradename =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X --> | pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category = | pregnancy_category =
| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> | legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> | legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status = | legal_status =
| routes_of_administration = | routes_of_administration =


<!--Pharmacokinetic data--> <!--Pharmacokinetic data-->
Line 21: Line 23:
| protein_bound = | protein_bound =
| metabolism = | metabolism =
| excretion = | excretion =


<!--Identifiers--> <!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = | CAS_number = 164025-33-6
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 9D3DS54YCD
| ATC_prefix = | ATC_prefix =
| ATC_suffix = | ATC_suffix =
| PubChem = 9971547 | PubChem = 9971547
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 45346
| DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = | DrugBank =
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 8147139


<!--Chemical data--> <!--Chemical data-->
| C=14 | H=14 | Cl=1 | N=3 | O=2 | C=14 | H=14 | Cl=1 | N=3 | O=2
| smiles = ClC1=CC=C2C(C(N(CC3=C(COC)N=CN32)C)=O)=C1
| molecular_weight = 291.732 g/mol
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| smiles = c3c(Cl)ccc-1c3C(=O)N(C)Cc2n-1cnc2COC
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = FXIDXTIMKAEBGY-UHFFFAOYSA-N
}} }}


'''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> '''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==
* ]
* ]
* ] * ]
* ] * ]


== References == ==References==
{{reflist}} {{Reflist}}


{{GABA receptor modulators}}
{{Benzodiazepines}} {{Benzodiazepines}}
{{Psychostimulants, agents used for ADHD and nootropics}}
{{GABAergics}}


] ]
] ]
] ]
⚫ ]
] ]
] ]
⚫ ]




{{nervous-system-drug-stub}} {{Nervous-system-drug-stub}}

Latest revision as of 17:15, 17 January 2025

Chemical compound Pharmaceutical compound
PWZ-029
Identifiers
IUPAC name
  • 8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazobenzodiazepin-6-one
CAS Number
PubChem CID
ChemSpider
UNII
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)


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