L-838,417

Catalog #: 3250
3 Citations Datasheet / COA / SDS

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L-838,417 | CAS No. 286456-42-6 | GABA-A Receptor Agonists

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Description: GABAA partial agonist; displays subtype selectivity

Chemical Name: 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

Purity: ≥98%

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Product Details

Citations (3)

Reviews

Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

L-838,417 is a subtype-selective GABA_A receptor partial agonist. Selectively binds to α1, α2, α3 and α5 subunits (K_i values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.

Technical Data

M.Wt:

399.4

Formula:

C₁₉H₁₉F₂N₇O

Solubility:

Soluble to 50 mM in DMSO

Purity:

≥98%

Storage:

Store at +4°C

CAS No:

286456-42-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:

Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)

Background References

Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABA_A receptors.
Soderhielm et al.
Biochem.Pharmacol., 2018;158:339
Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour.
McCabe et al.
Neuropharmacology, 2004;46:171
Differential behavioural effects of low efficacy positive GABA_A modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys.
McMahon and France
Br.J.Pharmacol., 2006;147:260
Reversal of pathological pain through specific spinal GABA_A receptor subtypes.
Knabl et al.
Nature, 2008;451:330

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Citations for L-838,417

The citations listed below are publications that use Tocris products. Selected citations for L-838,417 include:

3 Citations: Showing 1 - 3

Blockade of spinal α5-GABA_A receptors differentially reduces reserpine-induced fibromyalgia-type pain in female rats.
Authors: De la Luz-Cuellar Et al.
Eur J Pharmacol 2019;858:172443
Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABA_A receptors.
Authors: Soderhielm Et al.
Biochem Pharmacol 2018;158:339
Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia.
Authors: Gee Et al.
J Pharmacol Exp Ther 2010;332:1040

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