L-838,417

L-838,417 is a partial agonist of α₂-, α₃-, and α₅ subunit-containing GABA_A receptors.¹ It potentiates GABA-induced currents in LTK- cells expressing α₂β₃γ₂, α₃β₃γ₂, or α₅β₃γ₂ subunit-containing GABA_A receptors when used at a concentration of 100 nM. In vivo, L-838,417 (10 mg/kg) increases the mechanical paw withdrawal threshold in a rat model of spinal nerve ligation-induced static allodynia.² It also decreases social avoidance in a novel environment in adult and adolescent rats, indicating anxiolytic-like activity, when administered at doses of 1 and 2 mg/kg, respectively.³

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1. McKernan, R.M., Rosahl, T.W., Reynolds, D.S., et al. Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA_A receptor α1 subtype. Nat. Neurosci. 3(6), 587-592 (2000).

2. Nickolls, S., Mace, H., Fish, R., et al. A comparison of the α2/3/5 selective positive allosteric modulators L-838,417 and TPA023 in preclinical models of inflammatory and neuropathic pain. Adv. Pharmacol. Sci. 608912 (2011).

3. Morales, M., Varlinskaya, E.I., and Spear, L.P. Anxiolytic effects of the GABA_A receptor partial agonist, L-838,417: Impact of age, test context familiarity, and stress. Pharmacol. Biochem. Behav. 109, 31-37 (2013).