Cat. No.: HY-11018

Risperidone

(Synonyms: R 64 766)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

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Pureté: 99.87%
CAS No.: 106266-06-2
Formule: C₂₃H₂₇FN₄O₂
Masse moléculaire:410.48

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Risperidone Chemical Structure

CAS No.: 106266-06-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
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Activité biologique

Description

IC₅₀ & Target

D₂ Receptor

5.9 nM (Ki)

5-HT_2A Receptor

4.8 nM (Ki)

P-Glycoprotein

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	34.2 μM Compound: risperidone	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	[PMID: 23812503]
HEK293	IC₅₀	102 μM Compound: Risperidone	Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA	[PMID: 21300721]
HEK293	IC₅₀	125 μM Compound: Risperidone	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit	[PMID: 22761000]
HEK293	IC₅₀	1.6 μM Compound: risperidone	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	11 μM Compound: risperidone	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	291 μM Compound: risperidone	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	581 nM Compound: Risperidone	Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay	[PMID: 23675993]
HEK293	IC₅₀	>600 μg/mL Compound: Risperidone	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability Cytotoxicity against human HEK293 cells assessed as reduction in cell viability	[PMID: 32122737]
Ventricular myocyte	IC₅₀	73 μM Compound: Risperidone	Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes	[PMID: 21300721]
WI-38	CC₅₀	25 μM Compound: Risperidone	Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay	[PMID: 17893158]
WI-38	EC₅₀	>25 μM Compound: Risperidone	Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay	[PMID: 17893158]

In Vitro

Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively. Risperidone dose-dependently inhibited the release of IL-12 in mature DCs, while the production of IL-10 is dose-dependently increased by Risperidone. A high dose of risperidone can induce TNF-α release from mature DCs^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In the first experiment, body weight is found to be slightly but significantly lower in the Risperidone-treated rats as a function of age. Similar to the first experiment, age-dependent differences in body weight are also observed between the three treatment groups in the second locomotor experiment. Rats treated with the 3.0 mg/kg dose of Risperidone weigh less than vehicle-treated rats on postnatal days 35, 38, and 41. The third locomotor experiment involves larger, mixed-sex litters in contrast to the smaller, single-sex litters used in the first two experiments. As noted for the first two experiments, rats treated with Risperidone in the third experiment gain less weight in an age-dependent manner^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 106266-06-2
Appearance Solid
Masse moléculaire 410.48
Formule C₂₃H₂₇FN₄O₂
Color White to off-white
SMILES

O=C1C(CCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)=C(C)N=C5N1CCCC5
Synonyms

R 64 766
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (6)

All In Vivo Efficacy StudyBio/Physico-chemical AssayRT-PCRWB

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Journal Impact Factor

Emerg Contam

2026 Feb 23.
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
Int J Nanomedicine

Nano Parthenolide Improves Intestinal Barrier Function of Sepsis by Inhibiting Apoptosis and ROS via 5-HTR2A. [Abstract]

2023 Feb 11:18:693-709. PMID: 36816330
Front Pharmacol

Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment. [Abstract]

2023 Apr 21:14:1161964. PMID: 37153799

Risperidone purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]

Risperidone (0.1 mg/kg, p.o.; 0.1 ml/g) or aripiprazole also reduced MK801-induced schizophrenia-like behavior, 50B had a lower impact on reducing the distance mice traveled compared with risperidone, but had similar effects compared with aripiprazole.

Risperidone purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]

Risperidone (1 or 5 mg/kg, p.o.; 0.1 ml/10 g). 50A and 50B did not induce catalepsy in male mouse bar test. Results are expressed as mean ± SD (n = 5–6).
Eur J Pharm Sci

Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]

2023 Aug 1:187:106475. PMID: 37225005

Risperidone purchased from MedChemExpress. Usage Cited in: Eur J Pharm Sci. 2023 Aug 1:187:106475. [Abstract]

Reversible inhibition of CYP2J2 metabolism of arachidonic acid (AA) to 14,15-epoxyeicosatrienoic acid (14,15-EET) by Risperidone (0-20 μM).
Psychoneuroendocrinology

Chronic intranasal oxytocin alleviates cognitive impairment and reverses oxytocin signaling upregulation in MK801-induced mice. [Abstract]

2024 Oct:168:107138. PMID: 39068687

Risperidone purchased from MedChemExpress. Usage Cited in: Psychoneuroendocrinology. 2024 Oct:168:107138. [Abstract]

Risperidone (0.3 mg/kg, i.p.). Expression of OT signaling related genes in the hippocampus. RT-PCR (n=8–10) analysis were performed on brain tissues from the hippocampus of each group. The mRNA level of CD38, OTR and OT in the hippocampus are presented.

Risperidone purchased from MedChemExpress. Usage Cited in: Psychoneuroendocrinology. 2024 Oct:168:107138. [Abstract]

Expression of OT signaling related genes in the hippocampus. Western blot (n=6–8) analysis were performed on brain tissues from the hippocampus of each group. Western blot images and quantification of the band intensity compared to the basal level.

Solvant et solubilité

In Vitro:

DMSO : 10 mg/mL (24.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4362 mL

12.1809 mL

24.3617 mL

5 mM

0.4872 mL

2.4362 mL

4.8723 mL

10 mM

0.2436 mL

1.2181 mL

2.4362 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.44 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (2.44 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.44 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Protocole

Animal Administration^[4]

Rats^[4]
A total of 211 Long-Evans rats (56 females and 155 males) are used. Within each study, three groups of roughly equal numbers of rats receive injections of 1.0 mg/kg of Risperidone, 3.0 mg/kg of Risperidone, or the vehicle used for the Risperidone solution as a control. In the first experiment, twenty-six male rats (n=9 in the vehicle and 3.0 mg/kg Risperidone groups; n=8 in the 1.0 mg/kg Risperidone group) are tested for locomotor activity for 20 minutes a day beginning at postnatal day 49 and continuing daily until postnatal day 53. A second experiment determined if the locomotor effects of early-life Risperidone treatment persisted well into adulthood. A third experiment ascertains the effects of sex on the locomotor effects of early-life Risperidone seen in young adult rats. In this experiment, sixty male (n=20 per treatment group) and 56 female (n=19 rats in the vehicle and 3.0 mg/kg dose group, n=18 in the 1.0 mg/kg dose group) rats are treated. A fourth experiment assessed reversal learning during adulthood in rats administered earlylife risperidone. Forty-two male rats (n=14 per treatment group) are treated^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (419 KB)
- English - EN (419 KB)
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- Norwegian - NO (419 KB)
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- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Nyberg S, et al. 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology (Berl). 1993;110(3):265-72. [Content Brief]

[2]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cell apoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. [Content Brief]

[3]. Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. [Content Brief]

[4]. Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4362 mL	12.1809 mL	24.3617 mL	60.9043 mL
	5 mM	0.4872 mL	2.4362 mL	4.8723 mL	12.1809 mL
	10 mM	0.2436 mL	1.2181 mL	2.4362 mL	6.0904 mL
	15 mM	0.1624 mL	0.8121 mL	1.6241 mL	4.0603 mL
	20 mM	0.1218 mL	0.6090 mL	1.2181 mL	3.0452 mL

Keywords

Risperidone

6 Cited Publications

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Risperidone

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Publications Citing Use of MedChemExpress (MCE) Risperidone

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Voir tous les produits spécifiques à Isoform Dopamine Receptor

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Risperidone Related Classifications

Cat. No.: HY-11018