Paliperidone (9-Hydroxyrisperidone): A dopamine D2 and Serotonin 5-HT2 Receptors Antagonist
Paliperidone (another name: 9-hydroxyrisperidone), a benzisoxazole derivative, is acts as a dopamine type 2 (D
2) and serotonin type 2 (5-HT
2) receptors antagonist, and the major active metabolite of risperidone [
R0087]. Similarly to risperidone, paliperidone has also affinity for α
1- and α
2-adrenergic, and H
1 histaminergic receptors. Paliperidone has no affinity for cholinergic muscarinic or β
1- and β
2-adrenergic receptors. The pharmacological activity of the (+)- and (-)-paliperidone enantiomers is qualitatively and quantitatively similar
in vitro. Risperidone is used as an antipsychotic agent with relatively few side effects. Recently, paliperidone extended-release formulation is developed for clinical use. (The product is for research purpose only.)