| Field | Specification |
|---|---|
| Target | |
| Alternative names | R 64 766 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H27FN4O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Risperidone is a serotonin 5-HT2 receptor blocker, a P-glycoprotein inhibitor, and a potent dopamine D2 receptor antagonist, with Ki values of 4.8 nM and 5.9 nM at the 5-HT2A and dopamine D2 receptors, respectively. It is supplied as a white to off-white solid (C23H27FN4O2, MW 410.48) at 99.87% purity, and is also known as R 64 766.
Physical & Chemical Properties
| CAS Number | 106266-06-2 |
|---|---|
| Molecular Formula | C23H27FN4O2 |
| Molecular Weight | 410.48 g/mol |
| Purity | 99.87% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C1C(CCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)=C(C)N=C5N1CCCC5 |
| Target | D 2 Receptor, 5-HT 2A Receptor, P-Glycoprotein |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling; Membrane Transporter/Ion Channel |
| Solubility | In Vitro: DMSO: 10 mg/mL (24.36 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
|
D2 Receptor 5.9 nM (Ki) |
5-HT2A Receptor |
5-HT2A Receptor 4.8 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 10 mg/mL (24.36 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1 mg/mL (2.44 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1 mg/mL (2.44 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 1 mg/mL (2.44 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Risperidone blocks the serotonin 5-HT2 receptor, inhibits P-Glycoprotein, and is a potent antagonist of the dopamine D2 receptor, with Kis of 4.8 and 5.9 nM at 5-HT2A and the dopamine D2 receptor, respectively. In mature DCs, Risperidone dose-dependently inhibited IL-12 release while dose-dependently increasing IL-10 production. TNF-α release from mature DCs can be induced by a high dose of risperidone[3].
In Vivo
In the first experiment, body weight is slightly but significantly lower in Risperidone-treated rats across age. Age-dependent body weight differences among the three treatment groups are also seen in the second locomotor experiment, as in the first. On postnatal days 35, 38, and 41, rats given the 3.0 mg/kg dose of Risperidone weigh less than vehicle-treated rats. The third locomotor experiment uses larger, mixed-sex litters, unlike the smaller, single-sex litters of the first two experiments. As in the first two experiments, Risperidone-treated rats in the third experiment gain less weight in an age-dependent manner[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[4]
Rats[4] Use 211 Long-Evans rats (56 females and 155 males) in total. Within every study, split the animals into three groups of roughly equal size and inject 1.0 mg/kg of Risperidone, 3.0 mg/kg of Risperidone, or, as control, the vehicle in which the Risperidone solution is prepared. First experiment: record locomotor activity of twenty-six male rats (n=9 per group for the vehicle and 3.0 mg/kg Risperidone treatments; n=8 for the 1.0 mg/kg Risperidone treatment) for 20 minutes daily, starting at postnatal day 49 and ending at postnatal day 53. Second experiment: determine whether the effect of early-life Risperidone treatment on locomotion remains present into adulthood. Third experiment: establish how sex influences that locomotor effect in young adult rats, treating sixty male rats (n=20 per treatment group) and 56 female rats (vehicle group and 3.0 mg/kg dose group, n=19 rats each; 1.0 mg/kg dose group, n=18). Fourth experiment: evaluate reversal learning in adulthood after earlylife risperidone administration, treating forty-two male rats (n=14 per treatment group)[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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