RS-102221 hydrochloride

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CAS NO:

187397-18-8

RS-102221 hydrochloride 是一种选择性5-HT2C受体拮抗剂 (K_i=10 nM)。RS-102221 hydrochloride 对5-HT2C受体的选择性是5-HT2A和5-HT2B受体的近 100 倍。RS-102221 hydrochloride 能够促进新生神经细胞分化。RS-102221 hydrochloride 增加了大鼠的食物摄入量和体重增加。

生物活性

RS-102221 hydrochloride is a selective5-HT2C receptorantagonist (K_i=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the5-HT2C receptoras compared to the5-HT2Aand5-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].

IC₅₀& Target^[1]

5-HT_2CReceptor

10 nM (Ki)

5-HT_2AReceptor

5-HT_2BReceptor

体外研究
(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.

体内研究
(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]。

分子量

649.08

Formula

C₂₇H₃₂ClF₃N₄O₇S

CAS 号

187397-18-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.