Description
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
Product information
CAS Number: 286456-42-6
Molecular Weight: 399.40
Formula: C19H19F2N7O
Chemical Name: 5-({[7-tert-butyl-3-(2,5-difluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]oxy}methyl)-1-methyl-1H-1,2,4-triazole
Smiles: CN1N=CN=C1COC1=NN2C(=NN=C2C=C1C(C)(C)C)C1=CC(F)=CC=C1F
InChiKey: BQDUNOMMYOKHEP-UHFFFAOYSA-N
InChi: InChI=1S/C19H19F2N7O/c1-19(2,3)13-8-15-24-25-17(12-7-11(20)5-6-14(12)21)28(15)26-18(13)29-9-16-22-10-23-27(16)4/h5-8,10H,9H2,1-4H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. L-838417 (2.0 mg/kg) eliminates social avoidance, but has no anxiolytic effects on social investigation. 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.
References:
- Ciara McCabe, et al. Subtype-selective GABAergic drugs facilitate extinction of mouse operant behavior. Neuropharmacology. 2004 Feb;46(2):171-8.
- Melissa Morales, et al. Anxiolytic effects of the GABAA receptor partial agonist, L-838,417: Impact of age, test context familiarity, and stress. Pharmacol Biochem Behav. 2013 Aug;109:31-7.
Products are for research use only. Not for human use.
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