For research use only.

Catalog No.S1615 Synonyms: R-64766

1 publication

Risperidone  Chemical Structure

CAS No. 106266-06-2

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

Selleck's Risperidone has been cited by 1 publication

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Biological Activity

Description Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
5-HT2A [7] α2c-adrenergic receptor [7] D2 receptor [7] D3 receptor [7] D2L Receptor [7]
0.17 nM(Ki) 1.3 nM(Ki) 3.57 nM(Ki) 3.6 nM(Ki) 4.16 nM(Ki)
In vitro

Risperidone binds to both DA and serotonin (5HT) receptors, particularly in the neurons of striatal and limbic structures. Risperidone significantly affects brain nerve growth factor (NGF) level suggesting that it influences the turnover of endogenous growth factors. Risperidone significantly decreases BDNF concentrations in frontal cortex, occipital cortex and hippocampus and decreases or increases TrkB receptors in selected brain structures. [1] Risperidone significantly increases D(2) binding in medial prefrontal cortex by 34% in rat forebrain regions. Risperidone produces even greater up-regulation of D(4) receptors in CPu (37%), NAc (32%), and HIP (37%) in rat forebrain regions. [2] Risperidone significantly inhibits the production of NO and proinflammatory cytokines by activated microglia. [3] Risperidone (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. [4]

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. Risperidone significantly increases BWG and FI in female rats. [5] Risperidone (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. Risperidone (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.[6]


Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (9.74 mM)
Ethanol 4 mg/mL (9.74 mM)
Water Insoluble

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Chemical Information

Molecular Weight 410.48


CAS No. 106266-06-2
Storage powder
in solvent
Synonyms R-64766
Smiles CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04567524 Recruiting Drug: LYN-005 Schizophrenia Schizoaffective Lyndra Inc.|Worldwide Clinical Trials August 13 2020 Phase 2
NCT03978832 Completed Drug: PERSERIS|Drug: Risperidone Schizophrenia Indivior Inc. June 28 2019 Phase 4
NCT03503318 Completed Drug: TV-46000|Drug: Placebo Schizophrenia Teva Branded Pharmaceutical Products R&D Inc.|Teva Pharmaceutical Industries April 27 2018 Phase 3
NCT03302364 Unknown status Drug: Risperidone Schizophrenia|Mental Illness Cui Yimin|Peking University First Hospital October 22 2017 --

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