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Risperidone 5-HT Receptor antagonist

Cat.No.S1615

Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
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Quality Control

Batch: Purity: 99.54%
99.54

Solubility

In vitro
Batch:

Ethanol : 4 mg/mL

DMSO : 3 mg/mL (7.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 410.48 Formula

C23H27FN4O2

Storage (From the date of receipt)
CAS No. 106266-06-2 Download SDF Storage of Stock Solutions

Synonyms R-64766 SMILES CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
5-HT2A
0.17 nM(Ki)
α2c-adrenergic receptor
1.3 nM(Ki)
D2 receptor
3.57 nM(Ki)
D3 receptor
3.6 nM(Ki)
D2L Receptor
4.16 nM(Ki)
D4 receptor
4.66 nM(Ki)
D2S Receptor
4.73 nM(Ki)
α1A-adrenergic receptor
5 nM(Ki)
5-HT7
6.6 nM(Ki)
α1B-adrenergic receptor
9 nM(Ki)
5-HT2C
12 nM(Ki)
5-HT1B
14.9 nM(Ki)
α2a-adrenergic receptor
16.5 nM(Ki)
H1 receptor
20.1 nM(Ki)
5-HT2B
61.9 nM(Ki)
5-HT1D
84.6 nM(Ki)
α2b-adrenergic receptor
108 nM(Ki)
H2 receptor
120 nM(Ki)
5-HT5A
206 nM(Ki)
5-HT5A
206 nM(Ki)
D1 receptor
244 nM(Ki)
D5 receptor
290 nM(Ki)
In vitro

Risperidone binds to both DA and serotonin (5HT) receptors, particularly in the neurons of striatal and limbic structures. This compound significantly affects brain nerve growth factor (NGF) level suggesting that it influences the turnover of endogenous growth factors. It significantly decreases BDNF concentrations in frontal cortex, occipital cortex and hippocampus and decreases or increases TrkB receptors in selected brain structures. This chemical significantly increases D(2) binding in medial prefrontal cortex by 34% in rat forebrain regions. It produces even greater up-regulation of D(4) receptors in CPu (37%), NAc (32%), and HIP (37%) in rat forebrain regions. This compound significantly inhibits the production of NO and proinflammatory cytokines by activated microglia. It (1-50 mM) significantly enhances the intracellular accumulation of Rh123 in Caco-2 cells by inhibiting P-gp activity with an IC(50) value of 5.87 mM.

In vivo

Risperidone does not significantly affect bodyweight gain (BWG), food intake(FI), glucose tolerance or leptin levels, even though prolactin and corticosterone are significantly elevated in male rats. This compound significantly increases BWG and FI in female rats. It (0.05 mg/kg) increases food intake and leptin gene expression in white adipose tissue (WAT), but the rate of bodyweight gain is not affected in rats. This compound (0.5 mg/kg) causes a reduction in bodyweight gain, as well as enhanced Ucp1 gene expression in BAT and serum prolactin concentrations in rats.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16936711/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12443990/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12366389/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-26)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07152184 NOT_YET_RECRUITING
Patient With Schizophrenia Spectrum Disorder; NLM Classification WM 203, Psychology:Schizophrenic Psychology; Schizophrenia Spectrum and Other Psychotic Disorders
University Hospital, Strasbourg, France
2026-10-01 PHASE2
NCT06969755 RECRUITING
Schizophenia Disorder
Northwell Health
2024-09-04 PHASE4
NCT07483294 RECRUITING
Psychosis; Acute
Northwell Health
2025-11-01 PHASE4
NCT07665073 NOT_YET_RECRUITING
Bipolar 1 Disorder
Pakistan Institute of Medical Sciences
2027-06 PHASE4
NCT07490353 RECRUITING
Depression - Major Depressive Disorder; Anhedonia
Medical University of Vienna
2025-11-01 PHASE1
NCT07047651 ACTIVE_NOT_RECRUITING
Treatment Resistant Schizophrenia; Treatment Resistant Bipolar Disorder
Dr. Stavroula Rakitzi
2025-06-04 PHASE4

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