Name | RS 102221 hydrochloride,8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dionehydrochloride |
---|---|
Synonyms |
N-{5-[5-(2,4-Dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl]-2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide
RS-102221 Benzenesulfonamide, N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)- |
Description | 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[1][2]. |
---|---|
Related Catalog | |
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 (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 (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 (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 |
Density | 1.5±0.1 g/cm3 |
---|---|
Boiling Point | 753.5ºC at 760 mmHg |
Molecular Formula | C27H32ClF3N4O7S |
Molecular Weight | 612.618 |
Flash Point | 409.5ºC |
Exact Mass | 612.186584 |
PSA | 151.52000 |
LogP | 3.75 |
Vapour Pressure | 4.8E-23mmHg at 25°C |
Index of Refraction | 1.604 |