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Paliperidone-d4 (Synonyms: 9-hydroxy Risperidone-d4)

Catalog No.GC47857 Copy One-Click Copy Product Info

An internal standard for the quantification of paliperidone

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Paliperidone-d4 Chemical Structure

Cas No.: 1020719-55-4

Size Price Stock Qty
500 μg
$243.00
In stock
1 mg
$462.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Paliperidone-d4

Paliperidone-d4 is intended for use as an internal standard for the quantification of paliperidone by GC- or LC-MS. Paliperidone is an atypical antipsychotic.1 It is an inverse agonist of dopamine D2 and D3 receptors (IC50s = 1 and 0.9 nM, respectively), as well as an antagonist at these receptors (Kis = 0.4 and 0.1 nM, respectively).2 Paliperidone also binds to α1- and α2-adrenergic receptors, histamine H1 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 10.1, 80, 3.4, 480, 19, 1.21, and 48 nM, respectively).3 It improves spatial working memory in a T-maze alternation task in a maternal immune activation mouse model of schizophrenia when administered at a dose of 0.05 mg/kg per day.1 Paliperidone is also an active metabolite of the atypical antipsychotic risperidone .3 Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.

1.MacDowell, K.S., Munarriz-Cuezva, E., Caso, J.R., et al.Paliperidone reverts Toll-like receptor 3 signaling pathway activation and cognitive deficits in a maternal immune activation mouse model of schizophreniaNeuropharmacology116196-207(2017) 2.Burstein, E.S., Ma, J., Wong, S., et al.Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonistJ. Pharmacol. Exp. Ther.315(3)1278-1287(2005) 3.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000)

Chemical Properties of Paliperidone-d4

Cas No. 1020719-55-4 SDF
Synonyms 9-hydroxy Risperidone-d4
Canonical SMILES OC1C(N2CCC1)=NC(C)=C(C([2H])([2H])C([2H])([2H])N3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)C2=O
Formula C23H23D4FN4O3 M.Wt 430.5
Solubility Chloroform: slightly soluble,DMSO: slightly soluble,Methanol: slightly soluble Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Paliperidone-d4

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3229 mL 11.6144 mL 23.2288 mL
5 mM 464.6 μL 2.3229 mL 4.6458 mL
10 mM 232.3 μL 1.1614 mL 2.3229 mL
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In vivo Formulation Calculator (Clear solution) of Paliperidone-d4

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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