Risperidone mesylate
Based on 6 publication(s) in Google Scholar
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
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- CAS. Nr.: 666179-96-0
- Formel: C24H31FN4O5S
- Molecular Weight:506.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Risperidone mesylate
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RT-PCR
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WB
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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5-HT2A Receptor 4.8 nM (Ki) |
D2 Receptor 5.9 nM (Ki) |
5-HT2A Receptor |
P-glycoprotein |
Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Risperidone dose-dependently inhibited the release of IL-12 in mature DCs, while the production of IL-10 is dose-dependently increased by Risperidone. A high dose of risperidone can induce TNF-α release from mature DCs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 666179-96-0
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Molecular Weight 506.59
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Formel C24H31FN4O5S
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SMILES
CS(=O)(O)=O.FC1=CC(ON=C2C3CCN(CCC(C(N(CCCC4)C4=N5)=O)=C5C)CC3)=C2C=C1
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Synonyms
R 64 766 mesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Int J Nanomedicine
Nano Parthenolide Improves Intestinal Barrier Function of Sepsis by Inhibiting Apoptosis and ROS via 5-HTR2A. [Abstract]2023 Feb 11:18:693-709. PMID: 36816330 -
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J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Front Pharmacol
Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment. [Abstract]2023 Apr 21:14:1161964. PMID: 37153799
Risperidone mesylate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]
Risperidone (0.1 mg/kg, p.o.; 0.1 ml/g) or aripiprazole also reduced MK801-induced schizophrenia-like behavior, 50B had a lower impact on reducing the distance mice traveled compared with risperidone, but had similar effects compared with aripiprazole.
Risperidone mesylate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]
Risperidone (1 or 5 mg/kg, p.o.; 0.1 ml/10 g). 50A and 50B did not induce catalepsy in male mouse bar test. Results are expressed as mean ± SD (n = 5–6).
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Eur J Pharm Sci
Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]2023 Aug 1:187:106475. PMID: 37225005
Risperidone mesylate purchased from MedChemExpress. Usage Cited in: Eur J Pharm Sci. 2023 Aug 1:187:106475. [Abstract]
Reversible inhibition of CYP2J2 metabolism of arachidonic acid (AA) to 14,15-epoxyeicosatrienoic acid (14,15-EET) by Risperidone (0-20 μM).
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Psychoneuroendocrinology
Chronic intranasal oxytocin alleviates cognitive impairment and reverses oxytocin signaling upregulation in MK801-induced mice. [Abstract]2024 Oct:168:107138. PMID: 39068687
Risperidone mesylate purchased from MedChemExpress. Usage Cited in: Psychoneuroendocrinology. 2024 Oct:168:107138. [Abstract]
Risperidone (0.3 mg/kg, i.p.). Expression of OT signaling related genes in the hippocampus. RT-PCR (n=8–10) analysis were performed on brain tissues from the hippocampus of each group. The mRNA level of CD38, OTR and OT in the hippocampus are presented.
Risperidone mesylate purchased from MedChemExpress. Usage Cited in: Psychoneuroendocrinology. 2024 Oct:168:107138. [Abstract]
Expression of OT signaling related genes in the hippocampus. Western blot (n=6–8) analysis were performed on brain tissues from the hippocampus of each group. Western blot images and quantification of the band intensity compared to the basal level.
Protokoll
Rats[4]
A total of 211 Long-Evans rats (56 females and 155 males) are used. Within each study, three groups of roughly equal numbers of rats receive injections of 1.0 mg/kg of Risperidone, 3.0 mg/kg of Risperidone, or the vehicle used for the Risperidone solution as a control. In the first experiment, twenty-six male rats (n=9 in the vehicle and 3.0 mg/kg Risperidone groups; n=8 in the 1.0 mg/kg Risperidone group) are tested for locomotor activity for 20 minutes a day beginning at postnatal day 49 and continuing daily until postnatal day 53. A second experiment determined if the locomotor effects of early-life Risperidone treatment persisted well into adulthood. A third experiment ascertains the effects of sex on the locomotor effects of early-life Risperidone seen in young adult rats. In this experiment, sixty male (n=20 per treatment group) and 56 female (n=19 rats in the vehicle and 3.0 mg/kg dose group, n=18 in the 1.0 mg/kg dose group) rats are treated. A fourth experiment assessed reversal learning during adulthood in rats administered earlylife risperidone. Forty-two male rats (n=14 per treatment group) are treated[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
[1]. Nyberg S, et al. 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology (Berl). 1993;110(3):265-72. [Content Brief]
[2]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cellapoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. [Content Brief]
[3]. Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. [Content Brief]
[4]. Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Risperidone mesylate Related Classifications
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