Paliperidone
Based on 3 publication(s) in Google Scholar
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.43%
- No. CAS: 144598-75-4
- Fòrmula: C23H27FN4O3
- Peso molecular:426.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Paliperidone
MoreVer todos los productos específicos de isoformas Dopamine Receptor
MoreVer todos los productos específicos de isoformas 5-HT Receptor
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
D2 Receptor |
α adrenergic receptor |
5-HT2A Receptor |
α1 adrenergic receptor |
α2 adrenergic receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
193.9 μM
Compound: paliperidone
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
In Vitro
Paliperidone (10-100 μM, 12-24 h) increase caspase-3 activity in neuroblastoma cells[5].
Paliperidone (50-200 μM, 3 h) may modulate Akt1/GSK3β pathway to effectively protect SK-N-SH cells from the damages induced by glutamatein[6].
Paliperidone (100 μM, 24 h) can protect SK-N-SH cells from apoptosis induced by glutamate[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-SH cells
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Concentration:50-200 μM
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Incubation Time:3 h
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Result:Increased cell viability at dose of 100 and 200 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 144598-75-4
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Appearance Solid
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Peso molecular 426.48
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Fòrmula C23H27FN4O3
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Color White to off-white
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SMILES
CC1=C(C(N2CCCC(C2=N1)O)=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(F)=C5
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Synonyms
9-Hydroxyrisperidone
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Molecules
Identification of Novel PPARγ Partial Agonists Based on Virtual Screening Strategy: In Silico and In Vitro Experimental Validation. [Abstract]2024 Oct 15;29(20):4881. PMID: 39459249 -
Solvente y solubilidad
In Vitro:
DMSO : 5 mg/mL (11.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (1.17 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.17 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mauri MC, Paletta S, Maffini M, et al. Clinical pharmacology of atypical antipsychotics: an update. EXCLI J. 2014;13:1163-1191. Published 2014 Oct 13. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
[5]. Gassó P, et al. Neurotoxic/neuroprotective activity of haloperidol, risperidone and paliperidone in neuroblastoma cells. Prog Neuropsychopharmacol Biol Psychiatry. 2012 Jan 10;36(1):71-7. [Content Brief]
[6]. Peng L, et al. Paliperidone protects SK-N-SH cells against glutamate toxicity via Akt1/GSK3β signaling pathway. Schizophr Res. 2014 Aug;157(1-3):120-7. [Content Brief]
[7]. Boyda HN, et al. A comparison of the metabolic side-effects of the second-generation antipsychotic drugs risperidone and paliperidone in animal models. PLoS One. 2021 Jan 28;16(1):e0246211. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3448 mL | 11.7239 mL | 23.4478 mL | 58.6194 mL |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6896 mL | 11.7239 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8619 mL |
Paliperidone Related Classifications
HY-A0019 Related Classifications
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