RS 102221

Names

[ Name ]:
RS 102221

[Synonym ]:
Benzenesulfonamide, N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-, hydrochloride (1:1)
N-{5-[5-(2,4-Dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl]-2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide hydrochloride (1:1)

Biological Activity

[Description]:

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[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT2C Receptor:10 nM (Ki)

5-HT2A Receptor

5-HT2B Receptor

[In Vitro]

RS102221 (0.3-300nM; 24 h) 促进小鼠成年海马神经前体细胞 (ahNPCs) 分化，并显著增加 MAP-2+ 细胞的百分比[1]。 Cell Differentiation Assay[1] Cell Line: Mouse adult hippocampal neural progenitor cells (ahNPCs) Concentration: 0.3, 1, 10, 30, 100, and 300 nM Incubation Time: 24 hours Result: Significantly increases the percentage of MAP-2+ cells at 10 nM.

[In Vivo]

RS-102221 hydrochloride (2 mg/kg; 腹腔注射; 每天 1 次, 共 14 天) 增加大鼠的食物摄入量和体重增加[2]。 RS-102221 hydrochloride (2 mg/kg; 腹腔注射; 单次剂量) 与 3,4-亚甲基二氧基-N-甲基苯丙胺 (MDMA 或“摇头丸”) 联合施用于小鼠，可在前 1 小时抑制 MDMA 诱导厌食症，和 MDMA 诱导的过度运动[3]。 RS-102221 hydrochloride (2 mg/kg; 腹腔注射; 单次剂量) 可减轻小鼠在光暗试验中的焦虑，并降低惊吓反射的幅度[4]。

[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.

[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.

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₃₂ClF₃N₄O₇S

[ Molecular Weight ]:
649.079

[ Exact Mass ]:
648.163208

Related Compounds

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