| Identification | Back Directory | [Name]
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine | [CAS]
252977-51-8 | [Synonyms]
TPA 023
7-tert-butyl-6-[(2-ethyl-1,2,4-triazol-3-yl)methoxy]-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine
1,2,4-Triazolo[4,3-b]pyridazine, 7-(1,1-dimethylethyl)-6-[(1-ethyl-1H-1,2,4-triazol-5-yl)methoxy]-3-(2-fluorophenyl)- | [Molecular Formula]
C20H22FN7O | [MDL Number]
MFCD29921350 | [MOL File]
252977-51-8.mol | [Molecular Weight]
395.43 |
| Chemical Properties | Back Directory | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
2.08±0.10(Predicted) | [color ]
White to off-white | [InChI]
1S/C20H22FN7O/c1-5-27-17(22-12-23-27)11-29-19-14(20(2,3)4)10-16-24-25-18(28(16)26-19)13-8-6-7-9-15(13)21/h6-10,12H,5,11H2,1-4H3 | [InChIKey]
QKIWQBLNTSQOLY-UHFFFAOYSA-N | [SMILES]
CC(C)(C)C1=CC2=NN=C(C3=CC=CC=C3F)N2N=C1OCC4=NC=NN4CC |
| Hazard Information | Back Directory | [Uses]
TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM. | [Biological Activity]
TPA023 is a highly potentfunctionally selective agonist for α2-α3-and α5GABAA receptors th at shows zero efficacy at a1GABAA subtypes. TPA023 exhibits anxiolytic and anticonvulsant effects in both animals and humans but lacks sedative effects and abuse potential. | [in vivo]
TPA023 displays good receptor occupancy, when administered orally to rats. The dose of TPA023 resulting in 50% occupancy of rat brain GABAA receptors is 0.42 mg/kg, with the corresponding plasma concentration being 25 ng/mL. TPA023 is also efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection at a dose of 10 mg/kg i.p. (84% occupancy), with the ED50 of 0.19-0.41 nM, for protection against tonic convulsions (1.4 mg/kg i.p.) corresponding to around 50% occupancy. TPA023 (3 mg/kg p.o. in 0.5% methyl cellulose) shows anxiolytic-like effect on rats[1]. TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys[2]. | [References]
[1] Atack JR. Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023. Adv Pharmacol. 2009;57:137-85 DOI:10.1016/S1054-3589(08)57004-9
[2] Castner SA, et al. Reversal of ketamine-induced working memory impairments by the GABAAalpha2/3 agonist TPA023. Biol Psychiatry. 2010 May 15;67(10):998-1001. DOI:10.1016/j.biopsych.2010.01.001 |
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