RS-102221
Based on 2 publication(s) in Google Scholar
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 185376-97-0
- Formula: C27H31F3N4O7S
- Molecular Weight:612.62
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RS-102221
MoreAll 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
5-HT2C Receptor |
5-HT2C Receptor 10 nM (Ki) |
5-HT2A Receptor |
5-HT2B Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.5 nM
Compound: RS 102221
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Displacement of [3H]mesuleregine from human recombinant 5-HT2C receptor expressed in HEK293 cells
Displacement of [3H]mesuleregine from human recombinant 5-HT2C receptor expressed in HEK293 cells
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[PMID: 26988801] |
| HEK293 | IC50 |
1.5 nM
Compound: RS-102221
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Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | IC50 |
1.5 x 10-9 M
Compound: RS-102221
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Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
In Vitro
RS-102221 (0.3-300nM; 24 h) promotes the differentiation of adult hippocampal neural precursor cells (ahNPCs) and significantly increases the percentage of MAP-2+ cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse adult hippocampal neural progenitor cells (ahNPCs)
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Concentration:0.3, 1, 10, 30, 100, and 300 nM
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Incubation Time:24 hours
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Result:Significantly increases the percentage of MAP-2+ cells at 10 nM.
In Vivo
RS-102221 (2 mg/kg; i.p.; single dose), combined with the 3,4-Methylenedioxy-N-methamphetamine (MDMA or 'ecstasy'), suppresses the MDMA-induced hypophagia for the first 1 h period, and also suppresses MDMA-induced hyperlocomotion in mice[3].
RS-102221 (2 mg/kg; i.p.; single dose) can reduce anxiety and reduce the amplitude of startle reflex in mice in light and dark test[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 185376-97-0
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Appearance Solid
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Molecular Weight 612.62
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Formula C27H31F3N4O7S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C(F)(F)F)C=C1)(NC2=CC(C(CCCCN(CC3)CCC3(NC(N4)=O)C4=O)=O)=C(OC)C=C2OC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Brain
Hippocampal excitation-inhibition balance underlies the 5-HT2C receptor in modulating depressive behaviours. [Abstract]2024 Nov 4;147(11):3764-3779. PMID: 38701344 -
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (40.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Bortolotto V, et al. Proneurogenic Effects of Trazodone in Murine and Human Neural Progenitor Cells. ACS Chem Neurosci. 2017 Sep 20;8(9):2027-2038. [Content Brief]
[2]. Bonhaus DW, et al. RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):621-9. [Content Brief]
[3]. Salzer I, et al. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca(2+)-activated chloride channels. Neuropharmacology. 2016 Nov;110(Pt A):277-286. [Content Brief]
[4]. Conductier G, et al. 3,4-N-methlenedioxymethamphetamine-induced hypophagia is maintained in 5-HT1B receptor knockout mice, but suppressed by the 5-HT2C receptor antagonist RS102221. Neuropsychopharmacology. 2005 Jun;30(6):1056-63. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6323 mL | 8.1617 mL | 16.3233 mL | 40.8083 mL |
| 5 mM | 0.3265 mL | 1.6323 mL | 3.2647 mL | 8.1617 mL | |
| 10 mM | 0.1632 mL | 0.8162 mL | 1.6323 mL | 4.0808 mL | |
| 15 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7206 mL | |
| 20 mM | 0.0816 mL | 0.4081 mL | 0.8162 mL | 2.0404 mL | |
| 25 mM | 0.0653 mL | 0.3265 mL | 0.6529 mL | 1.6323 mL | |
| 30 mM | 0.0544 mL | 0.2721 mL | 0.5441 mL | 1.3603 mL | |
| 40 mM | 0.0408 mL | 0.2040 mL | 0.4081 mL | 1.0202 mL |
RS-102221 Related Classifications
HY-101365 Related Classifications
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