Paliperidone

Paliperidone is an atypical antipsychotic. 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). Paliperidone also binds to alpha1- and alpha2-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). 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. Paliperidone is also an active metabolite of the atypical antipsychotic risperidone (Cay-13629). Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.Formal Name: 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one. CAS Number: 144598-75-4. Synonyms: 9-hydroxy Risperidone, RO76477. Molecular Formula: C23H27FN4O3. Formula Weight: 426.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml. lambdamax: 237, 279 nm. SMILES: OC1C(N2CCC1)=NC(C)=C(CCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)C2=O. InChi Code: InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3. InChi Key: PMXMIIMHBWHSKN-UHFFFAOYSA-N.