Risperidone (R-64766; Risperdal)

Alias: R-64766; R64766; Risperidone; Risperidal; R 64766
Cat No.:V0982 Purity: ≥98%
Risperidone (R-64766; R64766 and Risperdal), an marketed atypical antipsychotic, is a potent multi-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, it has been approved for use in the treatment of schizophrenia and bipolar disorder.
Risperidone (R-64766; Risperdal) Chemical Structure CAS No.: 106266-06-2
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Risperidone (R-64766; Risperdal):

  • Risperidone-d4 (R 64 766-d4)
  • Risperidone hydrochloride
  • Risperidone Mesylate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Risperidone (R-64766; R64766 and Risperdal), an marketed atypical antipsychotic, is a potent multi-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, it has been approved for use in the treatment of schizophrenia and bipolar disorder. In particular, striatal and limbic structure neurons exhibit DA and serotonin (5HT) receptor binding when taking risperidone. Endogenous growth factor turnover may be influenced by risperidone, as evidenced by its substantial effects on brain nerve growth factor (NGF) levels.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT2A ( Ki = 0.17 nM ); α2c-adrenergic receptor ( Ki = 1.3 nM ); α2c-adrenergic receptor ( Ki = 1.3 nM ); D2 receptor ( Ki = 3.57 nM ); D3 receptor ( Ki = 3.6 nM ); D2L Receptor ( Ki = 4.16 nM )
ln Vitro

In vitro activity: Risperidone binds to serotonin (5HT) and dopamine (DA) receptors, especially those found in the neurons of the limbic and striatal regions. Risperidone dramatically alters the amount of brain nerve growth factor (NGF), indicating that it has an impact on endogenous growth factor turnover. Risperidone either increases or decreases TrkB receptors in specific brain structures and significantly reduces BDNF concentrations in the hippocampus, occipital cortex, and frontal cortex.[1] In rat forebrain regions, risperidone dramatically increases D(2) binding by 34% in the medial prefrontal cortex. In rat forebrain regions, risperidone causes an even higher up-regulation of D(4) receptors in CPu (37%), NAc (32%), and HIP (37%).[2] Risperidone dramatically reduces activated microglia's ability to produce proinflammatory cytokines and NO.[3] Risperidone (1-50 mM) increases the intracellular accumulation of Rh123 in Caco-2 cells by IC(50) = 5.87 mM, which is the inhibitory effect of P-gp activity. [4]

ln Vivo
Risperidone does not significantly impact leptin levels, glucose tolerance, bodyweight gain (BWG), or food intake (FI), despite the fact that prolactin and corticosterone are markedly increased in male rats. In female rats, risperidone dramatically raises BWG and FI.[5] In white adipose tissue (WAT), risperidone (0.05 mg/kg) increases food intake and leptin gene expression; however, it has no effect on the rate of bodyweight gain in rats. In rats, risperidone (0.5 mg/kg) reduces bodyweight gain and increases serum prolactin concentrations and Ucp1 gene expression in BAT.[6]
Animal Protocol
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).
Rats
References

[1]. J Neurosci Res . 2000 Jun 15;60(6):783-94.

[2]. J Pharmacol Exp Ther . 2001 May;297(2):711-7.

[3]. Schizophr Res,?007, 92(1-3), 108-115.

[4]. Neuropsychopharmacology . 2007 Apr;32(4):757-64.

[5]. Brain Res . 2002 Dec 6;957(1):144-51.

[6]. Clin Exp Pharmacol Physiol . 2002 Nov;29(11):980-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H27FN4O2
Molecular Weight
410.48
Exact Mass
410.21
Elemental Analysis
C, 67.30; H, 6.63; F, 4.63; N, 13.65; O, 7.80
CAS #
106266-06-2
Appearance
Solid powder
SMILES
CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
InChi Key
RAPZEAPATHNIPO-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H27FN4O2/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,2-4,7-13H2,1H
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
Synonyms
R-64766; R64766; Risperidone; Risperidal; R 64766
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 Data
Solubility (In Vitro)
DMSO: 4~10 mg/mL (9.7~24.4 mM)
Water: <1 mg/mL
Ethanol: ~4 mg/mL (~9.7 mM)
Preparing Stock Solutions 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

*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.

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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.
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Clinical Trial Information
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
Biological Data
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