Paliperidone

Model:144598-75-4

Paliperidone (3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one), also known as 9-hydroxyrisperidone, is the primary active metabolite of the atypical antipsychotic risperidone. Structurally, Paliperidone features a benzisoxazole ring system fused to a piperidine ring, connected via an ethyl linker to a tetrahydropyridopyrimidinone core bearing a hydroxy group at the 9-position.

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Product Description

Paliperidone is an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. Paliperidone is the 9-hydroxy metabolite of risperidone and exhibits high affinity for 5-HT₂A receptors (Ki = 0.4 nM for cloned human 5-HT₂A receptors) and potent dopamine D₂ receptor antagonism. Paliperidone is the active pharmaceutical ingredient in Invega® extended-release tablets for the treatment of schizophrenia and schizoaffective disorder. Paliperidone is also the active moiety released from Paliperidone Palmitate (Invega Sustenna®, Invega Trinza®) long-acting injectable suspensions. In quality control contexts, Paliperidone is officially designated as Risperidone Impurity C (EP), making it an essential analytical reference standard for impurity profiling in risperidone-containing products.

Product Parameters

Parameter	Specification
Product Name	Paliperidone
CAS Number	144598-75-4
Molecular Formula	C₂₃H₂₇FN₄O₃
Molecular Weight	426.48 g/mol
Melting Point	158–160°C
Boiling Point	612.3 ± 65.0 °C (Predicted)
Density	1.45 ± 0.1 g/cm³ (Predicted)
pKa	13.00 ± 0.60
Solubility	DMSO: soluble 2 mg/mL, clear (warmed)
Appearance	White to brown powder
Storage Condition	2–8°C

Application

Paliperidone is a chemical substance, the active metabolite of risperidone, an atypical antipsychotic drug. It is a scientific research reagent widely used in molecular biology, pharmacology and other scientific research fields. Paliperidone is a derivative of benzisoxazole, the active metabolite of risperidone, 9-hydroxyrisperidone, and a new type of antipsychotic drug. Its mechanism of action is still not fully understood, which may be related to the blocking effect on dopamine D2 and 5-hydroxytryptamine 2A (5HT2A). It has a blocking effect on adrenergic α1, α2 and histamine H1 receptors, and has no affinity for choline and adrenergic β1 and β2 receptors. Its levorotatory and dextrorotatory isomers have similar pharmacological effects in vitro

In Vitro Study

Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. Paliperidone acts well on Aβ (25-35) and MPP(+) at low concentrations (10 and 50 μM), and only protects SH-SY5Y from hydrogen peroxide damage. Paliperidone (100 μM) completely reduces cell loss induced by different stresses, independent of its dose. Paliperidone has a higher oxidative stress-scavenging effect than other APDs in many aspects, such as producing a large amount of glutathione, lower HNE, and protein carbonyl products. Paliperidone enhances dopamine toxicity at the highest dose, and is the only AP that significantly increases cell activity compared to cells treated with dopamine alone (8.1%）.

In Vivo Studies

Paliperidone restores extracellular glutamate in the basal layer of the prefrontal cortex of rats. In rats, Paliperidone also prevents the increase in extracellular glutamate induced by acute MK-801. The co-administration of Paliperidone and Escitalopram restores the inhibition of the firing rate of NE neurons and the percentage of sudden neuronal discharges. Paliperidone reduces biting and aggressive behaviors in a dose-dependent manner at effective doses. Paliperidone leads to a significant reduction in aggressive behaviors.

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Need Paliperidone as an API starting material, a Risperidone Impurity C reference standard, or a synthetic precursor to Paliperidone Palmitate? Cosperpharm supplies this active moiety with the analytical rigor and supply flexibility that regulatory filings demand. Our dedicated customer support team offers personalized assistance – from technical advice on storage and handling to custom documentation for your method validation or ANDA submission.

We welcome inquiries at any scale: reference standards, pilot batches, or bulk API quantities. Request a quote, ask about our stability monitoring program, or schedule a facility audit – our team is ready to assist. Contact Cosperpharm by email or through our website, and expect a clear, detailed proposal within one business day. Your success with Paliperidone starts with our commitment to quality and service.

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