RS-102221 hydrochloride|cas:187397-18-8|西域试剂

RS-102221 hydrochloride

产品编号：Bellancom-101365A| CAS NO：187397-18-8| 分子式：C₂₇H₃₂ClF₃N₄O₇S| 分子量：649.08

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货号	价格	库存与货期
Bellancom-101365A	￥1300.00	杭州北京（现货）
Bellancom-101365A	￥2100.00	杭州北京（现货）
Bellancom-101365A	￥4200.00	杭州北京（现货）
Bellancom-101365A	￥6800.00	杭州北京（现货）
Bellancom-101365A	￥10800.00	杭州北京（现货）

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RS-102221 hydrochloride

产品介绍

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 selective 5-HT2C receptor antagonist (K_i=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.

体外研究

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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Differentiation Assay

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。
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。
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]。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

溶解性数据

In Vitro:

DMSO : 125 mg/mL (192.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5406 mL	7.7032 mL	15.4064 mL
5 mM	0.3081 mL	1.5406 mL	3.0813 mL
10 mM	0.1541 mL	0.7703 mL	1.5406 mL

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.

参考文献

. 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]

. 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]

. 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]

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