Paliperidone

製品コードS1724 バッチS172401

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₃H₂₇FN₄O₃
	分子量	426.48	CAS No.	144598-75-4
Solubility (25°C)*	体外	5%TFA	15 mg/mL (35.17 mM)
		DMSO	Insoluble
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.
in vitro	Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. ^[1] Paliperidone works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protects SH-SY5Y from hydrogen peroxide. Paliperidone (100 μM) completely diminishes cell reduction induced by different stressors, regardless of their dosages. Paliperidone is demonstrated with higher oxidative stress-scavenging properties than other APDs in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions. ^[2] Paliperidone enhances dopamine toxicity at the highest dose and is the only AP that significantly increases cell viability (8.1%) compared with cells treated with dopamine alone. ^[3]
in vivo	Paliperidone normalizes prefrontal cortical basal extracellular glutamate in rats. Paliperidone also prevents the acute MK-801-induced increase in extracellular glutamate in rats. ^[4] Paliperidone coadministered with Escitalopram restores the suppression of the NE neuronal firing rate (n = 5 rats) and the percentage of neurons exhibiting burst firing. ^[5] Paliperidone results in a dose-dependent decrease in bite and attack behaviors with an effective dose. Paliperidone results in the maximal reduction in aggressive behavior. ^[6]

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904]	PubMed: 36386620
A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697]	PubMed: 33517273

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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