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- TPA-023 abstract "TPA-023 is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It is a subtype-selective, mixed agonist-antagonist at GABAA receptors, which acts as a partial agonist at the α2 and α3 subtypes, but as a silent antagonist at α1 and α5 subtypes. It has primarily anxiolytic and anticonvulsant effects in animal tests, but with no sedative effects even at 50× the effective anxiolytic dose.In human trials on healthy volunteers, TPA-023 was comparable to lorazepam, but had much less side effects on cognition, memory, alertness or coordination. In Phase II trials, the compound was significantly superior to placebo without inducing sedation. The clinical development was halted due to preclinical toxicity (cataract) in long term dosing studies. TPA-023 is well absorbed following oral administration and extensively metabolised by the liver, with a half-life of 6.7 hours. The main enzyme involved in its metabolism is CYP3A4, with some contribution by CYP3A5.".
- TPA-023 iupacName "7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine".
- TPA-023 thumbnail TPA-023.png?width=300.
- TPA-023 wikiPageID "18768096".
- TPA-023 wikiPageLength "5788".
- TPA-023 wikiPageOutDegree "18".
- TPA-023 wikiPageRevisionID "641627519".
- TPA-023 wikiPageWikiLink Anticonvulsant.
- TPA-023 wikiPageWikiLink Anxiolytic.
- TPA-023 wikiPageWikiLink Benzodiazepine.
- TPA-023 wikiPageWikiLink CYP3A4.
- TPA-023 wikiPageWikiLink CYP3A5.
- TPA-023 wikiPageWikiLink Category:Anxiolytics.
- TPA-023 wikiPageWikiLink Category:Ethers.
- TPA-023 wikiPageWikiLink Category:GABAA_receptor_positive_allosteric_modulators.
- TPA-023 wikiPageWikiLink Category:Organofluorides.
- TPA-023 wikiPageWikiLink Category:Triazoles.
- TPA-023 wikiPageWikiLink Category:Triazolopyridazines.
- TPA-023 wikiPageWikiLink GABAA_receptor.
- TPA-023 wikiPageWikiLink Lorazepam.
- TPA-023 wikiPageWikiLink Nonbenzodiazepine.
- TPA-023 wikiPageWikiLink Partial_agonist.
- TPA-023 wikiPageWikiLink Receptor_antagonist.
- TPA-023 wikiPageWikiLink Sedative.
- TPA-023 wikiPageWikiLinkText "TPA-023".
- TPA-023 alt "Ball-and-stick model of the TPA-023 molecule".
- TPA-023 c "20".
- TPA-023 eliminationHalfLife "24120.0".
- TPA-023 f "1".
- TPA-023 h "22".
- TPA-023 image "TPA-023 3D ball.png".
- TPA-023 iupacName "7".
- TPA-023 metabolism "hepatic".
- TPA-023 molecularWeight "395.432".
- TPA-023 n "7".
- TPA-023 o "1".
- TPA-023 routesOfAdministration "oral".
- TPA-023 smiles "CCC2=Cc3nncn3N=C2OCc4ncnn4CC".
- TPA-023 verifiedrevid "448183034".
- TPA-023 width "240".
- TPA-023 wikiPageUsesTemplate Template:Anxiolytics.
- TPA-023 wikiPageUsesTemplate Template:Drugbox.
- TPA-023 wikiPageUsesTemplate Template:GABAAR_PAMs.
- TPA-023 wikiPageUsesTemplate Template:Reflist.
- TPA-023 subject Category:Anxiolytics.
- TPA-023 subject Category:Ethers.
- TPA-023 subject Category:GABAA_receptor_positive_allosteric_modulators.
- TPA-023 subject Category:Organofluorides.
- TPA-023 subject Category:Triazoles.
- TPA-023 subject Category:Triazolopyridazines.
- TPA-023 hypernym Drug.
- TPA-023 type ChemicalSubstance.
- TPA-023 type Drug.
- TPA-023 type Group.
- TPA-023 type Azole.
- TPA-023 type Chemical.
- TPA-023 type Ether.
- TPA-023 type Group.
- TPA-023 type Heterocycle.
- TPA-023 type Organofluoride.
- TPA-023 type Organohalide.
- TPA-023 type Organofluoride.
- TPA-023 type Organohalide.
- TPA-023 type ChemicalObject.
- TPA-023 type Thing.
- TPA-023 type Q8386.
- TPA-023 comment "TPA-023 is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It is a subtype-selective, mixed agonist-antagonist at GABAA receptors, which acts as a partial agonist at the α2 and α3 subtypes, but as a silent antagonist at α1 and α5 subtypes.".
- TPA-023 label "TPA-023".
- TPA-023 sameAs Q7671096.
- TPA-023 sameAs m.04gj68z.
- TPA-023 sameAs TPA-023.
- TPA-023 sameAs TPA-023.
- TPA-023 sameAs Q7671096.
- TPA-023 wasDerivedFrom TPA-023?oldid=641627519.
- TPA-023 depiction TPA-023.png.
- TPA-023 isPrimaryTopicOf TPA-023.