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Paliperidone

Description Metabolism Pharmacology Uses Mechanism of Action
Paliperidone
Paliperidone structure
CAS No.
144598-75-4
Chemical Name:
Paliperidone
Synonyms
r76477;RO 76477;iperidone;Paliperidone;Palliperidone;Paliperidoner;Paliperidone I;Paliperidone>Racemic Paliperidone;9-HYDROXYRISPERIDONE
CBNumber:
CB9222359
Molecular Formula:
C23H27FN4O3
Formula Weight:
426.48
MOL File:
144598-75-4.mol

Paliperidone Properties

Melting point:
158-160°C
Boiling point:
612.3±65.0 °C(Predicted)
Density 
1.45±0.1 g/cm3(Predicted)
Flash point:
9℃
storage temp. 
2-8°C
solubility 
DMSO: soluble2mg/mL, clear (warmed)
pka
13.00±0.60(Predicted)
form 
powder
color 
white to brown
CAS DataBase Reference
144598-75-4(CAS DataBase Reference)
FDA UNII
838F01T721
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS02,GHS06,GHS08
Signal word  Danger
Hazard statements  H225-H301+H311+H331-H370-H301
Precautionary statements  P210-P260-P280-P301+P310-P311
Hazard Codes  T,F
Risk Statements  25-39/23/24/25-23/24/25-11
Safety Statements  45-36/37-16
RIDADR  UN 2811 6.1/PG 3
WGK Germany  3
RTECS  UV1164720
HazardClass  6.1
PackingGroup  III
HS Code  29349990

Paliperidone price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich H-076 9-Hydroxyrisperidone solution 1.0mg/mL in methanol, ampule of 1mL, certified reference material 144598-75-4 076-1ml $158 2020-08-18 Buy
Sigma-Aldrich H-076 9-Hydroxyrisperidone solution 1.0?mg/mL in methanol, ampule of 1?mL, certified reference material, Cerilliant? 144598-75-4 1 mL $163 2021-03-22 Buy
Sigma-Aldrich 1491809 Paliperidone United States Pharmacopeia (USP) Reference Standard 144598-75-4 200mg $812 2021-03-22 Buy
TCI Chemical P1897 Paliperidone >97.0%(T) 144598-75-4 200mg $186 2021-03-22 Buy
TCI Chemical P1897 Paliperidone >97.0%(T) 144598-75-4 1g $648 2021-03-22 Buy

Paliperidone Chemical Properties,Uses,Production

Description

Paliperidone, (±)-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(Invega), is essentially insoluble in water and is available asextended-release tablets. Paliperidone is delivered at a constantrate using an osmotic drug release device (OsmoticRelease Oral Systems [OROS]). Paliperidone is FDA-approved for schizophrenia aged 12–17. However, the pharmacologic portfolio, extrapolation from adult studies, and the long track record of the parent drug, risperidone in child/adolescent psychiatric (CAP) population might expand its therapeutic potential.

Metabolism

Paliperidone is the primary active metabolite of risperidone. The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006.

Pharmacology

Paliperidone , 9-hydroxyrisperidone, is an atypical antipsychotic, a serotonin (5HT2A) dopamine (D2) antagonist and the active metabolite of the high-potency risperidone. It has also 5HT7 antagonism that might confer some antidepressant actions. It is advantageous given the osmotic-controlled release oral delivery system technique facilitating once-daily dosing, rapid steady-state, and hence better compliance. Moreover, lack of cytochrome CYP-450 enzyme interactions, more alpha-2 affinity, alleged less propensity for extrapyramidal syndromes, and availability of long-acting injection formulation all render paliperidone a very appealing treatment option in psychoses and in hepatic patients too.

Uses

This medication is used to treat certain mental/mood disorders (such as schizophrenia, schizoaffective disorder). This medication can decrease hallucinations and help you to think more clearly and positively about yourself, feel less agitated, and take a more active part in everyday life. Paliperidone belongs to a class of drugs called atypical antipsychotics. It works by helping to restore the balance of certain natural substances in the brain.

Mechanism of Action

Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.

Description

Paliperidone, the C-9 hydroxylated active metabolite of the antipsychotic agent risperidone, is the newest atypical antipsychotic to join the market following the introductions of olanzapine (ZyprexaTM), risperidone (RisperdalTM), quetiapine(SeroquelTM),
and ziprasidone (GeodonTM). Compared to its parent, paliperidone has improved PK properties and a reduced potential for drug interactions. In terms of receptor affinity, the two drugs are equipotent.

Chemical Properties

Off White to Light Orange Coloured Solid

Originator

Johnson & Johnson (US)

Uses

A metabolite of Risperidone, a combined serotonin (5-HT2) and dopamine (D2) receptor antagonist

Uses

A metabolite of Risperidone (R525000), a combined serotonin (5-HT2) and dopamine (D2) receptor antagonist.

Uses

Paliperidone(Invega) is an atypical antipsychotic. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone. It is indicated for the acute and maintenance treatment of schizophrenia

brand name

Invega

General Description

Paliperidone, (±)-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(Invega), is essentially insoluble in water and is available asextended-release tablets. Paliperidone is delivered at a constantrate using an osmotic drug release device (OsmoticRelease Oral Systems [OROS]). The absolute bioavailabilityof paliperidone is 28%, and studies in healthy subjects on ahigh-fat, high-calorie meal showed an increase in AUC.Paliperidone is 74% bound to plasma proteins. After a single,1-mg dose of C-paliperidone, 59% of the dose was excretedin the urine as unchanged drug, and 32% of the dose was recoveredas metabolites. Most of the drug (80%) is excreted bythe kidneys. Paliperidone is metabolized by dealkylation, hydroxylation,dehydrogenation, and scission of the benzoxazolering. None of these metabolic pathways account for morethan 10% of the dose. The terminal elimination half-life ofpaliperidone is 23 hours.

Side effects

The most common adverse events included tachycardia, QTc prolongation, headache, anxiety, dizziness, tremors, and insomnia along with the dose-related events of somnolence, orthostatic hypotension, salivary hypersecretion, and extrapyrimidal disorder. Weight gain was also observed in 6–9% of patients which may be attributable to paliperidone’s lower affinity for H1-histaminergic and a1- and a2-adrenergic receptors. Patients with renal impairment require dose adjustments since elimination of paliperidone is altered. Paliperidone is contraindicated in patients with a hypersensitivity to risperidone. Concomitant use of class III antiarrhythmic agents should be avoided since this may result in additive QT interval prolongation. Also, loss of levodopa efficacy is expected with this D2 antagonist.

Chemical Synthesis

The synthesis of paliperidone involves the reaction of 2-acetyl-g-butyrolactone with 2-amino-3-benzyloxypyridine in the presence of phosphoryl chloride. The benzyl protecting group of the intermediate 9-benzyloxy- 3-(2-chloroethyl)-2-methylpyrido[1,2-a]pyrimidin-4-one is then removed by hydrogenolysis over Pd/C followed by the nucleophilic displacement of the chlorine with 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole to provide racemic paliperidone. While paliperidone can be resolved, both enantiomers are equipotent and interconvert in vivo obviating the need for separation.

Paliperidone Preparation Products And Raw materials

Raw materials

Preparation Products


Paliperidone Suppliers

Global( 333)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20010 60
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8882 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3245 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3013 60
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29961 58
Tianjin Huiren Chemtech Co., Ltd
86-13672008665
86-22-23707858 huirentech@foxmail.com CHINA 110 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28229 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 linda@hubeijusheng.com CHINA 23035 58

Related articles


View Lastest Price from Paliperidone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-10-14 Paliperidone
144598-75-4
US $15.00 / KG 1KG 99% 9000kg/per week Hebei Lingding Biological Technology Co., Ltd
2021-09-14 Paliperidone
144598-75-4
US $111.10 / g 10g 99% 80kg Baoji Guokang Healthchem co.,ltd
2021-07-20 Paliperidone
144598-75-4
US $0.00-0.00 / KG 5mg 99% HPLC 2000tons Shaanxi Dideu Medichem Co. Ltd

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