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666179-96-0

中文名稱 666179-96-0
英文名稱 Risperidone (Mesylate)
CAS 666179-96-0
分子式 C24H31FN4O5S
分子量 506.59
MOL 文件 666179-96-0.mol
666179-96-0 結(jié)構(gòu)式 666179-96-0 結(jié)構(gòu)式

基本信息

中文別名
利哌酮甲磺酸鹽
英文別名
Risperidone (Mesylate)
APEXIDONE
R-64766
R64766

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)粉末

常見問題列表

生物活性
Risperidone mesylate(R 64 766 mesylate) 是 5-HT2 受體的阻斷劑,P-糖蛋白 (P-Glycoprotein) 的抑制劑 和 dopamine D2 受體的拮抗劑,其對 5-HT2A 和 dopamine D2 受體的 Ki 值分別為 4.8,5.9 nM。
靶點(diǎn)

5-HT 2A Receptor

4.8 nM (Ki)

Dopamine D 2 receptor

5.9 nM (Ki)

P-glycoprotein

體外研究

Risperidone is a serotonin 5-HT 2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D 2 receptor antagonist, with K i s of 4.8, 5.9 nM for 5-HT 2A and dopamine D 2 receptor, respectively. Risperidone dose-dependently inhibited the release of IL-12 in mature DCs, while the production of IL-10 is dose-dependently increased by Risperidone. A high dose of risperidone can induce TNF-α release from mature DCs.

體內(nèi)研究

In the first experiment, body weight is found to be slightly but significantly lower in the Risperidone-treated rats as a function of age. Similar to the first experiment, age-dependent differences in body weight are also observed between the three treatment groups in the second locomotor experiment. Rats treated with the 3.0 mg/kg dose of Risperidone weigh less than vehicle-treated rats on postnatal days 35, 38, and 41. The third locomotor experiment involves larger, mixed-sex litters in contrast to the smaller, single-sex litters used in the first two experiments. As noted for the first two experiments, rats treated with Risperidone in the third experiment gain less weight in an age-dependent manner.

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