Home Neuronal Signaling 5-HT Receptor antagonist Risperidone For research use only.

Risperidone

Synonyms: R-64766

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

Risperidone Chemical Structure

Risperidone Chemical Structure

CAS No. 106266-06-2

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Risperidone Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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.
Targets
5-HT2A [7] α2c-adrenergic receptor [7] D2 receptor [7] D3 receptor [7] D2L Receptor [7] Click to View More Targets
0.17 nM(Ki) 1.3 nM(Ki) 3.57 nM(Ki) 3.6 nM(Ki) 4.16 nM(Ki)
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06218979 Recruiting
Psychosis|Food-drug Interaction
Helsinki University Central Hospital|University of Helsinki
 December 4 2023 Phase 1
NCT05710237 Recruiting
Treatment-resistant Depression
Centre for Addiction and Mental Health
 July 1 2023 Phase 2
NCT05374356 Unknown status
Post-Operative Confusion
University of Manitoba
 May 2022 Not Applicable
NCT04567524 Completed
Schizophrenia Schizoaffective
Lyndra Inc.|Worldwide Clinical Trials
 August 13 2020 Phase 2
NCT03978832 Completed
Schizophrenia
Indivior Inc.
 June 28 2019 Phase 4

Chemical Information & Solubility

Molecular Weight 410.48 Formula

C23H27FN4O2
CAS No. 106266-06-2 SDF Download Risperidone SDF
Smiles CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 4 mg/mL

DMSO : 3 mg/mL ( (7.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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