tcsc0020804 Ocaperidone

Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT₂ and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.

IC50 & Target: Ki: 0.14 nM (5HT₂), 0.46 nM (a₁-adrenergic receptor), 0.75 nM (Dopamine D₂), 1.6 nM (Histamine H₁), 5.4 nM (a₂-adrenergic receptor)^[1]


pEC50: 7.60 (h5-HT_1A)^[2]


pKi: 8.08 (h5-HT_1A)^[2]

In Vitro: Ocaperidone has high affinify at 5-HT₂ and dopamine D₂, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5HT₂, a₁-adrenergic, dopamine D₂, histamine H₁ and a₂-adrenergic, respectively^[1]. Ocaperidone shows 5-HT_1A receptor agonist activity, with a pEC₅₀ and pK_i of 7.60 and 8.08^[2].

In Vivo: Ocaperidone shows a potent occupation of 5HT₂ receptor via in vivo binding in the frontal cortex of rats with an ED₅₀ of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D₂ receptor in the striatum and the nucleus accumbens^[1]. Ocaperidone (R 79598) antagonizes dopamine D₂ and 5-HT₂, and shows a a partial generalization to buspirone with an ED₅₀ of 0.163 mg/kg^[3].