Name | Paliperidone |
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Synonyms |
UNII:838F01T721
4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl- 9-OH-risperidone 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one 9-Hydroxyrisperidone 3-{2-[4-(6-Fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one Paliperidone MFCD00871802 3-{2-[4-(6-Fluoro-1,2-benzoxazol-3-yl)-1-piperidinyl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one |
Description | Paliperidone (9-hydroxyrisperidone) is a dopamine antagonist of the atypical antipsychotic class of medications. IC50 value:Target: dopamine receptorin vitro: Paliperidone inhibited MK-801 induced neurotoxicity both in MTT metabolism assay (p<0.01) and in lactate dehydrogenase (LDH) activity assay (p<0.01). Moreover, paliperidone could significantly retard MK-801-mediated inhibition of neurite outgrowth (p<0.01) and reverse MK-801-induced decreases of gene expression and phosphorylation of Akt1 and GSK3β (both p<0.01). Furthermore, these protective effects of paliperidone were blocked by pretreatment with a PI3K inhibitor LY294002 [1]. paliperidone works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protected SH-SY5Y from hydrogen peroxide. At 100 μM, paliperidone completely diminished cell reduction induced by different stressors, regardless of their dosages. Paliperidone was demonstrated with a higher oxidative stress-scavenging properties than other APDs in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions [2].in vivo: The 9OHRIS (4 mg/bwkg) was administred by gastric tube. Four groups were formed depending on the treatment: (1) control, (2) stress, (3) 9OHRIS, (4) stress and parallel 9OHRIS treatment (n=5-6). The expression of APP, MAPK1, β-actin mRNAs from the perfused brain samples was measured with real-time PCR technique [3].Male offspring were treated orally via drinking water with vehicle, risperidone (0.01mg/kg/day), or paliperidone (0.01mg/kg/day) between postnatal days 35 and 56 (periadolescence) and extracellular glutamate levels in the prefrontal cortex were determined by microdialysis at PD 56 [4]. |
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Related Catalog | |
References |
Density | 1.5±0.1 g/cm3 |
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Boiling Point | 612.3±65.0 °C at 760 mmHg |
Melting Point | 158-160°C |
Molecular Formula | C23H27FN4O3 |
Molecular Weight | 426.484 |
Flash Point | 324.1±34.3 °C |
Exact Mass | 426.206726 |
PSA | 84.39000 |
LogP | 1.52 |
Vapour Pressure | 0.0±1.9 mmHg at 25°C |
Index of Refraction | 1.692 |
Storage condition | Room temp |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
Symbol |
GHS06 |
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Signal Word | Danger |
Hazard Statements | H301 |
Precautionary Statements | P301 + P310 |
Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
Hazard Codes | T: Toxic; |
Risk Phrases | R25 |
Safety Phrases | S45 |
RIDADR | UN 2811 6.1/PG 3 |
RTECS | UV1164720 |
Precursor 7 | |
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DownStream 2 | |