产品描述:
Paliperidone is an atypical antipsychotic.{42913} It is an inverse agonist of dopamine D2 and D3 receptors (IC50s = 1 and 0.9 nM, respectively), as well as an antagonist at these receptors (Kis = 0.4 and 0.1 nM, respectively).{25512} Paliperidone also binds to α1- and α2-adrenergic receptors, histamine H1 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 10.1, 80, 3.4, 480, 19, 1.21, and 48 nM, respectively).{25511} It improves spatial working memory in a T-maze alternation task in a maternal immune activation mouse model of schizophrenia when administered at a dose of 0.05 mg/kg per day.{42913} Paliperidone is also an active metabolite of the atypical antipsychotic risperidone (Item No. 13629).{25511} Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.