| Bioactivity | 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]. |
| Invitro | 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: |
| 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]。 |
| Name | RS-102221 |
| CAS | 185376-97-0 |
| Formula | C27H31F3N4O7S |
| Molar Mass | 612.62 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
RS-102221
CAS: 185376-97-0 F: C27H31F3N4O7S W: 612.62
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT
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