Clocapramine

Clocapramine is an antagonist of the D₂, 5-HT_2A receptors. IC50 & Target: D₂ and 5-HT_2A receptor^[1] In Vitro: Clocapramine has a moderate affinity for D₂-receptors in vitro. Clocapramine shows higher affinity for 5-HT_2A than for D₂-receptors in vitro^[1]. In Vivo: Clocapramine shows the lowest potency for D₂-occupancy in vivo^[1]. 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)^[2].