Risperidone

Catalog No.S1615 Synonyms: R-64766

Risperidone  Chemical Structure

Molecular Weight(MW): 410.48

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

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Biological Activity

Description Risperidone 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]
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]

Protocol

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 410.48
Formula

C23H27FN4O2

CAS No. 106266-06-2
Storage powder
Synonyms R-64766

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02926976 Not yet recruiting Schizophrenia Shanghai Mental Health Center November 2016 --
NCT02893371 Not yet recruiting Bipolar Disorder University of New Mexico|Patient-Centered Outcomes Research Institute|Montana State University|National Alliance on Mental Illness|CGStat LLC|Risk Benefit Statistics LLC September 2016 --
NCT02822092 Recruiting Psychotic Disorders Northwell Health July 2016 --
NCT02758067 Withdrawn Schizophrenia H. Lundbeck A/S|Otsuka Pharmaceutical Co., Ltd. June 2016 Phase 3
NCT02717195 Recruiting Schizophrenia H. Lundbeck A/S April 2016 Phase 3
NCT02773576 Active, not recruiting Schizophrenia Braeburn Pharmaceuticals April 2016 Phase 3

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID