| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Risperidone HCl is the hydrochloride salt of Risperidone (R64766; R-64766; Risperdal), which is an approved atypical antipsychotic for the treatment of schizophrenia and bipolar disorder.
| Targets |
5-HT2 Receptor ( Ki = 4.8 nM ); D2 Receptor ( Ki = 5.9 nM ); P-Glycoprotein
|
|---|---|
| ln Vitro |
Risperidone is a strong antagonist of the dopamine D2 receptor and a blocker of the serotonin 5-HT2 receptor. It is also an inhibitor of P-glycoprotein with Kis values of 4.8 and 5.9 nM for 5-HT2A and dopamine D2 receptors, respectively. Risperidone increases the production of IL-10 in mature DCs while dose-dependently inhibiting the release of IL-12. Risperidone at high dosages has the ability to cause mature DCs to release TNF-α[3].
|
| ln Vivo |
In the first trial, it was discovered that rats given risperidone had a slight but significant reduction in body weight as they aged. In the second exercise experiment, age-dependent weight differences were also noted among the three treatment groups. On postnatal days 35, 38, and 41, rats treated with 3.0 mg/kg of risperidone weighed less than rats given a vehicle. Compared to the smaller single-sex litter used in the first two locomotion experiments, a larger mixed-sex litter was used in the third experiment. In the third experiment, rats treated with risperidone gained less weight in an age-dependent manner, as was observed in the first two experiments [4].
|
| 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].
|
| References |
|
| Molecular Formula |
C₂₃H₂₈CLFN₄O₂
|
|---|---|
| Molecular Weight |
446.95
|
| Exact Mass |
446.188
|
| CAS # |
666179-74-4
|
| Related CAS # |
Risperidone; 106266-06-2; Risperidone mesylate; 666179-96-0
|
| PubChem CID |
9889802
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
31
|
| Complexity |
731
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].FC1C([H])=C([H])C2=C(C=1[H])ON=C2C1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C2=C(C([H])([H])[H])N=C3C([H])([H])C([H])([H])C([H])([H])C([H])([H])N3C2=O)C([H])([H])C1([H])[H]
|
| InChi Key |
OCBZQKQWVUTYDN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H27FN4O2.ClH/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;/h5-6,14,16H,2-4,7-13H2,1H3;1H
|
| 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;hydrochloride
|
| Synonyms |
R 64 766 hydrochloride; R-64 766; R64766
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2374 mL | 11.1869 mL | 22.3739 mL | |
| 5 mM | 0.4475 mL | 2.2374 mL | 4.4748 mL | |
| 10 mM | 0.2237 mL | 1.1187 mL | 2.2374 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 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
