Paliperidone

Modify Date: 2024-01-02 10:12:00

Paliperidone Structure
Paliperidone structure
 Common Name Paliperidone
CAS Number 144598-75-4 Molecular Weight 426.484
Density 1.5±0.1 g/cm3 Boiling Point 612.3±65.0 °C at 760 mmHg
Molecular Formula C23H27FN4O3 Melting Point 158-160°C
MSDS Chinese USA Flash Point 324.1±34.3 °C
Symbol GHS06
GHS06		 Signal Word Danger

 Use of Paliperidone


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].

 Names

Name Paliperidone
Synonym More Synonyms

 Paliperidone Biological Activity

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].
Related Catalog
References

[1]. Peng L, et al. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013 Jun;147(1):14-23.

[2]. Yang MC, et al. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011 Oct;217(3):397-410.

[3]. Kalman S, et al. 9-hydroxy-risperidone (9OHRIS) prevents stress-induced β-actin overexpression in rat hippocampus. Neuropsychopharmacol Hung. 2010 Sep;12(3):425-31.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
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

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UV1164720
CHEMICAL NAME :
4H-Pyrido(2,1-a)pyrimidin-4-one, 6,7,8,9-tetrahydro-3-(2-(4-(6-fluro-1,2-benzisoxazol- 3-yl)-1-piperidinyl)e thyl)-9-hydroxy-2-methyl-
CAS REGISTRY NUMBER :
144598-75-4
LAST UPDATED :
199509
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C23-H27-F-N4-O3
MOLECULAR WEIGHT :
426.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
65 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DDREDK Drug Development Research. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 33,399,1994

 Safety Information

Symbol GHS06
GHS06
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

 Synthetic Route

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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
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