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{{short description|Chemical compound}} |
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{{drugbox |
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{{Drugbox |
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| verifiedrevid = 405764220 |
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| Verifiedfields = changed |
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| IUPAC_name = 8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazobenzodiazepin-6-one |
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| Watchedfields = changed |
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| image = PWZ-029_structure.png |
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| verifiedrevid = 424715425 |
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| CAS_number = |
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| IUPAC_name = 8-chloro-3-(methoxymethyl)-5-methyl-4''H''-imidazobenzodiazepin-6-one |
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| ATC_prefix = |
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| image = PWZ-029.svg |
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| ATC_suffix = |
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| PubChem = 9971547 |
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<!--Clinical data--> |
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| DrugBank = |
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| tradename = |
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| C=14|H=14|Cl=1|N=3|O=2 |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| molecular_weight = 291.732 g/mol |
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| smiles = c3c(Cl)ccc-1c3C(=O)N(C)Cc2n-1cnc2COC |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category = |
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| bioavailability = |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| protein_bound = |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| metabolism = |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| elimination_half-life = |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| excretion = |
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| legal_status = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| routes_of_administration = |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category= |
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<!--Pharmacokinetic data--> |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| bioavailability = |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| protein_bound = |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| metabolism = |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| excretion = |
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| legal_status = |
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| routes_of_administration = |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 164025-33-6 |
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| ATC_prefix = |
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| ATC_suffix = |
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| PubChem = 9971547 |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = 45346 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = 8147139 |
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<!--Chemical data--> |
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| C=14 | H=14 | Cl=1 | N=3 | O=2 |
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| smiles = ClC1=CC=C2C(C(N(CC3=C(COC)N=CN32)C)=O)=C1 |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| 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 |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChIKey = FXIDXTIMKAEBGY-UHFFFAOYSA-N |
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}} |
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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. {{DOI|10.1016/j.brainres.2008.02.020}} PMID 18394590</ref> |
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'''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> |
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==See also== |
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==See also== |
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== References == |
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==References== |
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{{reflist}} |
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{{Reflist}} |
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{{GABA receptor modulators}} |
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{{Benzodiazepines}} |
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{{Benzodiazepines}} |
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{{Psychostimulants, agents used for ADHD and nootropics}} |
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{{GABAergics}} |
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{{nervous-system-drug-stub}} |
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{{Nervous-system-drug-stub}} |