Alpidem

Alpidem is an anxiolytic agent.¹ It selectively binds to α₁β₂γ₂ subunit-containing GABA_A receptors over α₅β₂γ₂ subunit-containing GABA_A receptors in HEK293 cells (IC₅₀s = 0.017 and ≥10 µM, respectively, for the recombinant rat receptors).² Alpidem also binds to the GABA_A/benzodiazepine receptor complex and translocator protein 18 kDa (TSPO) with IC₅₀ values of 0.028 and 0.0079 µM, respectively.³ It reduces marble burying in mice, indicating anxiolytic activity, with a minimum effective dose (MED) of 10 mg/kg.⁴ Unlike the benzodiazepine alprazolam, alpidem does not induce sedation in mice when administered at doses up to 2 mg/kg.⁵ Formulations containing alpidem have previously been used in the treatment of generalized anxiety disorder.

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1. Skolnick, P. Anxioselective anxiolytics: On a quest for the holy grail. Trends Pharamacol. Sci. 33(11), 611-620 (2012).

2. Faure-Halley, C., Graham, D., Arbilla, S., et al. Expression and properties of recombinant α1β₂γ2 and α5β₂γ2 forms of the rat GABA_A receptor. Eur. J. Pharmacol. 246(3), 283-287 (1993).

3. Trapani, G., Franco, M.C., Ricciardi, L., et al. Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type. J. Med. Chem. 40(19), 3109-3118 (1997).

4. Zivkovic, B., Morel, E., Joly, D., et al. Pharmacological and behavioral profile of alpidem as an anxiolytic. Pharmacopsychiatry 23(Suppl. 3), 108-113 (1990).

5. Hascoët, M., and Bourin, M. Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in rats. Pharmacol. Biochem. Behav. 56(2), 317-324 (1997).