Home Neuronal Signaling 5-HT Receptor antagonist Risperidone

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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.
Risperidone 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 410.48

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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

Solubility

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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Mechanism of Action

Targets/IC50/Ki
5-HT2A [7]
0.17 nM(Ki)
α2c-adrenergic receptor [7]
1.3 nM(Ki)
D2 receptor [7]
3.57 nM(Ki)
D3 receptor [7]
3.6 nM(Ki)
D2L Receptor [7]
4.16 nM(Ki)
D4 receptor [7]
4.66 nM(Ki)
D2S Receptor [7]
4.73 nM(Ki)
α1A-adrenergic receptor [7]
5 nM(Ki)
5-HT7 [7]
6.6 nM(Ki)
α1B-adrenergic receptor [7]
9 nM(Ki)
5-HT2C [7]
12 nM(Ki)
5-HT1B [7]
14.9 nM(Ki)
α2a-adrenergic receptor [7]
16.5 nM(Ki)
H1 receptor [7]
20.1 nM(Ki)
5-HT2B [7]
61.9 nM(Ki)
5-HT1D [7]
84.6 nM(Ki)
α2b-adrenergic receptor [7]
108 nM(Ki)
H2 receptor [7]
120 nM(Ki)
5-HT5A [1]
206 nM(Ki)
5-HT5A [7]
206 nM(Ki)
D1 receptor [7]
244 nM(Ki)
D5 receptor [7]
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. [1] 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. [2] This compound significantly inhibits the production of NO and proinflammatory cytokines by activated microglia. [3] 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. [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. This compound significantly increases BWG and FI in female rats. [5] 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.[6]
References
  • https://pubmed.ncbi.nlm.nih.gov/16936711/
  • https://pubmed.ncbi.nlm.nih.gov/12443990/
  • https://pubmed.ncbi.nlm.nih.gov/12366389/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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