Risperidone
Risperidone is a benzisoxazole atypical antipsychotic that also exhibits antidepressant, anti-inflammatory, and neuroprotective activities. Risperidone acts as an antagonist at D2 receptors and 5-HT2A receptors and as an agonist at 5-HT7 receptors. In vivo, risperidone increases release of DA, 5-HT, and NE in the frontal cortex. Risperidone is also a partial uncompetitive inhibitor of D-amino acid oxidase, which inhibits oxidation of D-serine, an NMDA receptor agonist associated with the onset of schizophrenia; risperidone also inhibits D-amino acid-induced cell death in vitro. In animal models of neuroinflammation or encephalitis, risperidone increases expression of PPARγ and decreases LPS-induced expression of TNF-α, IL-1β, COX, p38 MAPK, and NF-κB.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18959810
| Cas No. |
106266-06-2 |
|---|---|
| Purity |
≥98% |
| Formula |
C23H27FN4O2 |
| Formula Wt. |
410.49 |
| Chemical Name |
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[2,1-b]pyrimidin-4-one |
| IUPAC Name |
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one |
| Melting Point |
170C |
| Appearance |
White Crystal Powder |
Kamińska K, Gołembiowska K, Rogóż Z. Effect of risperidone on the fluoxetine-induced changes in extracellular dopamine, serotonin and noradrenaline in the rat frontal cortex. Pharmacol Rep. 2013;65(5):1144-51. PMID: 24399710.
MacDowell KS, García-Bueno B, Madrigal JL, et al. Risperidone normalizes increased inflammatory parameters and restores anti-inflammatory pathways in a model of neuroinflammation. Int J Neuropsychopharmacol. 2013 Feb;16(1):121-35. PMID: 22176740.
Kozielska M, Johnson M, Pilla Reddy V, et al. Pharmacokinetic-pharmacodynamic modeling of the D2 and 5-HT (2A) receptor occupancy of risperidone and paliperidone in rats. Pharm Res. 2012 Jul;29(7):1932-48. PMID: 22437487.
Abou El-Magd RM, Park HK, Kawazoe T, et al. The effect of risperidone on D-amino acid oxidase activity as a hypothesis for a novel mechanism of action in the treatment of schizophrenia. J Psychopharmacol. 2010 Jul;24(7):1055-67. PMID: 19329549.
Toohey N, Klein MT, Knight J, et al. Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other “inactivating antagonists”. Mol Pharmacol. 2009 Sep;76(3):552-9. PMID: 19509219.
Potkin SG, Saha AR, Kujawa MJ, et al. Aripiprazole, an antipsychotic with a novel mechanism of action, and risperidone vs placebo in patients with schizophrenia and schizoaffective disorder. Arch Gen Psychiatry. 2003 Jul;60(7):681-90. PMID: 12860772.
Farde L, Nyberg S, Oxenstierna G, et al. Positron emission tomography studies on D2 and 5-HT2 receptor binding in risperidone-treated schizophrenic patients. J Clin Psychopharmacol. 1995 Feb;15(1 Suppl 1):19S-23S. PMID: 7537284.
