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Clocapramine is an antagonist of the D₂, 5-HT_2A receptors.

Clocapramine has a moderate affinity for D₂-receptors in vitro. Clocapramine shows higher affinity for 5-HT_2A than for D₂-receptors in vitro.

Clocapramine shows the lowest potency for D₂-occupancy in vivo. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D₂ and frontal serotonin-5-HT₂ receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT₂ versus D₂ receptors that fall between these two groups (ED₅₀ of 14.5 mg/kg for D₂, 4.9 mg/kg for 5-HT₂).

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