RS-102221 hydrochloride
Based on 2 publication(s) in Google Scholar
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats.
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 187397-18-8
- Formula: C27H32ClF3N4O7S
- Molecular Weight:649.08
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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 Citing Use of MedChemExpress (MCE) RS-102221 hydrochloride
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT2C Receptor |
5-HT2C Receptor 10 nM (Ki) |
5-HT2A Receptor |
5-HT2B Receptor |
RS-102221 hydrochloride (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.
RS-102221 hydrochloride (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 hydrochloride (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. 187397-18-8
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Appearance Solid
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Molecular Weight 649.08
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Formula C27H32ClF3N4O7S
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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.Cl
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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
DMSO : 125 mg/mL (192.58 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 (277 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 | 1.5406 mL | 7.7032 mL | 15.4064 mL | 38.5161 mL |
| 5 mM | 0.3081 mL | 1.5406 mL | 3.0813 mL | 7.7032 mL | |
| 10 mM | 0.1541 mL | 0.7703 mL | 1.5406 mL | 3.8516 mL | |
| 15 mM | 0.1027 mL | 0.5135 mL | 1.0271 mL | 2.5677 mL | |
| 20 mM | 0.0770 mL | 0.3852 mL | 0.7703 mL | 1.9258 mL | |
| 25 mM | 0.0616 mL | 0.3081 mL | 0.6163 mL | 1.5406 mL | |
| 30 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL | 1.2839 mL | |
| 40 mM | 0.0385 mL | 0.1926 mL | 0.3852 mL | 0.9629 mL | |
| 50 mM | 0.0308 mL | 0.1541 mL | 0.3081 mL | 0.7703 mL | |
| 60 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL | |
| 80 mM | 0.0193 mL | 0.0963 mL | 0.1926 mL | 0.4815 mL | |
| 100 mM | 0.0154 mL | 0.0770 mL | 0.1541 mL | 0.3852 mL |