L-838417
L-838417 Basic information
- Product Name:
- L-838417
- Synonyms:
-
- 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
- 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]-
- L-838417
- 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
- 5-({[7-tert-butyl-3-(2,5-difluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]oxy}methyl)-1-methyl-1,2,4-triazole
- L-838417_x000b_
- CAS:
- 286456-42-6
- MF:
- C19H19F2N7O
- MW:
- 399.4
- Product Categories:
-
- Heterocycles
- Intermediates & Fine Chemicals
- Heterocyclic Compounds
- Pharmaceuticals
- Mol File:
- 286456-42-6.mol
L-838417 Chemical Properties
- Melting point:
- 196-198°C
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at +4°C
- solubility
- DMSO: ≥20mg/mL
- pka
- 2.13±0.10(Predicted)
- form
- powder
- color
- white to off-white
L-838417 Usage And Synthesis
Chemical Properties
White to Off-White Solid
Uses
A selective ligand for GABAA receptors
Uses
L-838417 is an anxiolytic agent and a selective GABAA receptor partial agonist that selectively binds to α1, α2, α3 and α5 subunits (1,2). It also exhibits antinociceptive and anti-inflammatory properties.
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. |
storage
Store at +4°C
L-838417 Supplier
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