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.
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- CAS. Nr.: 185376-97-0
- Formel: C27H31F3N4O7S
- Molecular Weight:612.62
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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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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RS-102221
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Biologische Aktivität
Beschreibung
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 |
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| 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. Nr. 185376-97-0
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Molecular Weight 612.62
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Formel C27H31F3N4O7S
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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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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 (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 -
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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