Ocaperidone

• CAT Number: M118634
• CAS Number: 129029-23-8
• Molecular Formula: C24H25FN4O2
• Molecular Weight: 420.488
• Purity: ≥95%
• Target: D2 antagonist
• Storage: -20°C
• IUPAC Name: 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethylpyrido[1,2-a]pyrimidin-4-one
• InChI: InChI=1S/C24H25FN4O2/c1-15-4-3-10-29-23(15)26-16(2)19(24(29)30)9-13-28-11-7-17(8-12-28)22-20-6-5-18(25)14-21(20)31-27-22/h3-6,10,14,17H,7-9,11-13H2,1-2H3
• InChIKey: ZZQNEJILGNNOEP-UHFFFAOYSA-N
• SMILES: CC1=CC=CN2C1=NC(=C(C2=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F)C

Ocaperidone, also known as R 79598, is a highly potent and efficacious dopamine-D2 antagonist with concomitant, equivalent serotonin 5-HT2 antagonism. Ocaperidone inhibited dopamine agonist (apomorphine, amphetamine or cocaine)-induced behavioral effects at low doses (0.014-0.042 mg/kg). Ocaperidone completely blocked the dopamine agonist behavior at slightly higher doses (0.064 mg/kg). Ocaperidone is expected to exert pronounced haloperidol-like effects on the positive symptoms of schizophrenic patients but with risperidone-like low extrapyramidal side effect liability and improved patient compliance.

Reference

1:In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Leysen JE, Janssen PM, Gommeren W, Wynants J, Pauwels PJ, Janssen PA.Mol Pharmacol. 1992 Mar;41(3):494-508. PMID: 1372084 2:Behavioral disinhibition and depression in amphetaminized rats: a comparison of risperidone, ocaperidone and haloperidol. Megens AA, Niemegeers CJ, Awouters FH.J Pharmacol Exp Ther. 1992 Jan;260(1):160-7. PMID: 1370539 3:Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). Megens AA, Awouters FH, Meert TF, Schellekens KH, Niemegeers CJ, Janssen PA.J Pharmacol Exp Ther. 1992 Jan;260(1):146-59. PMID: 1370538