| Identification | Back Directory | [Name]
L-838417 | [CAS]
286456-42-6 | [Synonyms]
L-838417
7-(tert-Butyl)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine
1,2,4-Triazolo[4,3-b]pyridazine,3-(2,5-difluorophenyl)-7-(1,1-dimethylethyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-
3-(2,5-Difluorophenyl)-7-(1,1-dimethylethyl)-6-[(1-methyl-1H-1,2,4,-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine
3-(2,5-Difluorophenyl)-7-(1,1-dimethylethyl)-6-[(1-methyl-1H-1,2,4,-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-β]pyridazine | [Molecular Formula]
C19H19F2N7O | [MDL Number]
MFCD08690609 | [MOL File]
286456-42-6.mol | [Molecular Weight]
399.4 |
| Chemical Properties | Back Directory | [Appearance]
White to Off-White Solid | [Melting point ]
196-198°C | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [pka]
2.13±0.10(Predicted) | [color ]
white to off-white |
| Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Solid | [Uses]
A selective ligand for GABAA receptors | [Biological Activity]
Subtype-selective GABA A receptor partial agonist. Selectively binds to α 1, α 2, α 3 and α 5 subunits (K i values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α 1 ( α 1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo . | [in vivo]
L-838417 (1.0 mg/kg) produces anxiolytic effects in adult rat, as indexed by a transformation of social avoidance into preference and an increase in social investigation[2].
L-838417 (2.0 mg/kg) eliminates social avoidance, but has no anxiolytic effects on social investigation[2].
L-838417 (0.5 mg/kg) reverses the anxiogenic effects of prior stress regardless of age, but with doses ≥ 1 mg/kg decreases social investigation, an effect possibly due in part to locomotor-impairing effects of this compound[2].
| Animal Model: | Male and female adolescent and adult Sprague–Dawley rats[2]. | | Dosage: | 0, 0.5, 1.0, 2.0, or 4.0 mg/kg. | | Administration: | IP. | | Result: | Adolescents required a higher dose (2 mg/kg) to attenuate their social avoidance.
The lowest dose of 0.5 mg/kg was sufficient to reverse the anxiogenic effects of repeated restraint as reflected by a significant increase in the coefficient relative to vehicle-treated animals.
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| [storage]
Store at +4°C |
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