Opipramol

Opipramol is a sigma-1 (σ₁) and σ₂ receptor ligand.¹ It binds to σ₁ and σ₂ receptors in guinea pig brain membrane preparations (IC₅₀s = 7 and 56 nM, respectively). It is selective for σ₁ and σ₂ over histamine H₂, dopamine D₁, α₁- and α₂-adrenergic, and muscarinic M₁ receptors (IC₅₀s = 4,300, 900, 200, 6,100, and 3,300 nM, respectively) and has no effect on serotonin (5-HT) or norepinephrine uptake (IC₅₀s = >10,000 nM for both), but does bind to histamine H₁ and dopamine D₂ receptors (IC₅₀s = 12 and 120 nM, respectively), as well as the 5-HT receptor subtype 5-HT₂ (IC₅₀ = 120 nM). Opipramol (0.01 mg/kg) increases social interaction time in a social exploration test in rats, indicating anxiolytic-like activity. It also decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity, when administered at a dose of 10 mg/kg.

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1. Müller, W.E., Siebert, B., Holoubek, G., et al. Neuropharmacology of the anxiolytic drug opipramol, a sigma site ligand. Pharmacopsychiatry 37(Suppl 3), S189-S197 (2004).