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Risperidone 5-HT Receptor antagonist

Name: Risperidone
Brand: Selleck Chemicals
SKU: S1615
Availability: InStock
Rating: 5 (4 reviews)

Catalog No.S1615 Purity:99.54%

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

Chemical Structure

Molecular Weight: 410.48

Purity & Quality Control

Batch: Purity: 99.54%

99.54

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Signaling Pathway

5-HT Receptor Signaling Pathway

Mechanism of Action

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)	Click to View More Targets

In vitro
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

https://pubmed.ncbi.nlm.nih.gov/10861791/
https://pubmed.ncbi.nlm.nih.gov/11303062/
http://www.ncbi.nlm.nih.gov/pubmed/ 17363222

https://pubmed.ncbi.nlm.nih.gov/16936711/
https://pubmed.ncbi.nlm.nih.gov/12443990/
https://pubmed.ncbi.nlm.nih.gov/12366389/

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Chemical Information

Molecular Weight	410.48	Formula	C₂₃H₂₇FN₄O₂
CAS No.	106266-06-2	SDF	Download SDF
Synonyms	R-64766
Smiles	CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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