1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. 5-HT Receptor
    Dopamine Receptor
    P-glycoprotein
  3. Risperidone

Risperidone (Synonyms: R 64 766)

Cat. No.: HY-11018 Purity: 99.16%
Handling Instructions

Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

For research use only. We do not sell to patients.

Risperidone Chemical Structure

Risperidone Chemical Structure

CAS No. : 106266-06-2

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Description

Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

IC50 & Target

Ki: 4.8 nM (5-HT2A receptor); 5.9 nM (dopamine D2 receptor), P-Glycoprotein[1][2].

In Vitro

Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A 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].

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].

Clinical Trial
Molecular Weight

410.48

Formula

C₂₃H₂₇FN₄O₂

CAS No.

106266-06-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (24.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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].

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

References
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Keywords:

RisperidoneR 64 7665-HT ReceptorDopamine ReceptorP-glycoproteinSerotonin Receptor5-hydroxytryptamine ReceptorP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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