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Alpidem is an anxiolytic agent.1 It selectively binds to α1β2γ2 subunit-containing GABAA receptors over α5β2γ2 subunit-containing GABAA receptors in HEK293 cells (IC50s = 0.017 and ≥10 µM, respectively, for the recombinant rat receptors).2 Alpidem also binds to the GABAA/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. Anxioselective anxiolytics: On a quest for the holy grail. Trends Pharamacol. Sci. 33(11), 611-620 (2012).
2. Expression and properties of recombinant α1β2γ2 and α5β2γ2 forms of the rat GABAA receptor. Eur. J. Pharmacol. 246(3), 283-287 (1993).
3. Synthesis and binding affinity of 2-
4. Pharmacological and behavioral profile of alpidem as an anxiolytic. Pharmacopsychiatry 23(Suppl. 3), 108-113 (1990).
5. Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in rats. Pharmacol. Biochem. Behav. 56(2), 317-324 (1997).