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| 100mg |
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| 250mg |
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Risperidone mesylate is the mesylate salt of Risperidone (R64766; Risperdal), which is an approved atypical antipsychotic and a blocker of dopamine D2 receptors as well as serotonin 5-HT2 receptors.
| Targets |
5-HT2A Receptor ( Ki = 4.8 nM ); D2 Receptor ( Ki = 5.9 nM ); P-glycoprotein
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| ln Vitro |
Risperidone has a Kis of 4.8 and 5.9 nM for the 5-HT2A and D2 dopamine receptors, respectively, making it a strong antagonist of the dopamine receptor, a P-Glycoprotein inhibitor, and a blocker of the serotonin 5-HT2 receptor. In contrast to its dose-dependent induction of IL-10 production, risperidone inhibited the release of IL-12 in mature DCs. Maturated DCs may release TNF-α when given a high dose of risperidone[3].
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| ln Vivo |
In the initial trial, it was discovered that the rats given Risperidone had a marginally, but statistically significant, decreased body weight with increasing age. Age-dependent variations in body weight are also noted in the second locomotor experiment among the three treatment groups. Postnatal days 35, 38, and 41 weight loss is observed in rats given a 3.0 mg/kg dose of risperidone as opposed to rats given a vehicle. Larger, mixed-sex litters are used in the third locomotor experiment, as opposed to the smaller, single-sex litters utilized in the first two. In the third trial, rats given risperidone experienced a decrease in weight gain that was age-dependent, as was observed in the first two[4].
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| Animal Protocol |
Rats: A total of 211 Long-Evans rats are utilized, comprising 56 females and 155 males. Three groups of approximately equal numbers of rats are injected with either 1.0 mg/kg of risperidone, 3.0 mg/kg of risperidone, or the vehicle used to administer the risperidone solution as a control within each study. 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 used in the first experiment. They are tested for locomotor activity for 20 minutes every day starting on postnatal day 49 and continuing every day until postnatal day 53. The long-term effects of early-life Risperidone treatment on locomotion were examined in a follow-up study. In a third experiment, the effects of sex on early-life Risperidone's locomotor effects in young adult rats are investigated. Sixty male (n = 20 per treatment group) and fifty-six 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 in this experiment. In a fourth experiment, rats given risperidone early in life were evaluated for reversal learning during adulthood. Treatment is given to 42 male rats (n=14 per treatment group)[4].
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| References |
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| Molecular Formula |
C24H31FN4O5S
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|---|---|
| Molecular Weight |
506.59
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| Elemental Analysis |
C, 56.90; H, 6.17; F, 3.75; N, 11.06; O, 15.79; S, 6.33
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| CAS # |
666179-96-0
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| Related CAS # |
Risperidone; 106266-06-2; Risperidone hydrochloride; 666179-74-4
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F.CS(=O)(=O)O
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| InChi Key |
OJUQOWYTFBZUKJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27FN4O2.CH4O3S/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22;1-5(2,3)4/h5-6,14,16H,2-4,7-13H2,1H3;1H3,(H,2,3,4)
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| Chemical Name |
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one;methanesulfonic acid
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| Synonyms |
Risperidone Mesylate salt; Risperidone Mesylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9740 mL | 9.8699 mL | 19.7398 mL | |
| 5 mM | 0.3948 mL | 1.9740 mL | 3.9480 mL | |
| 10 mM | 0.1974 mL | 0.9870 mL | 1.9740 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04940039 | Active Recruiting |
Drug: Risperidone 3 mg Drug: Paliperidone Palmitate 50 mg eq. |
Schizophrenia | Janssen-Cilag International NV | July 22, 2021 | Phase 4 |
| NCT03522168 | Active Recruiting |
Drug: Risperidone Drug: Aripiprazole |
Weight, Body | Duke University | January 10, 2019 | N/A |
| NCT05480046 | Recruiting | Drug: Risperidone ISM | Schizophrenia | Rovi Pharmaceuticals Laboratories | October 18, 2022 | N/A |
| NCT05779241 | Recruiting | Drug: LYN-005 Drug: Risperidone |
Schizophrenia Schizoaffective Disorder |
Lyndra Inc. | April 2023 | Phase 3 |
| NCT05890768 | Recruiting | Drug: Lumateperone Drug: Risperidone |
Psychosis | University of New Mexico | May 11, 2023 | Phase 4 |
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