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666179-74-4

中文名称 666179-74-4
英文名称 Risperidone (hydrochloride)
CAS 666179-74-4
分子式 C23H28ClFN4O2
分子量 446.945
MOL 文件 666179-74-4.mol
666179-74-4 结构式 666179-74-4 结构式

基本信息

中文别名
利哌酮盐酸盐
英文别名
Risperidone (hydrochloride)
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜
形态粉末

常见问题列表

生物活性
Risperidone hydrochloride (R 64 766 hydrochloride) 是 5-HT2 受体的阻断剂,P-糖蛋白 (P-Glycoprotein) 的抑制剂 和 dopamine D2 受体的拮抗剂,其对 5-HT2A 和 dopamine D2 受体的 Ki 值分别为 4.8,5.9 nM。
靶点

5-HT 2 Receptor

4.8 nM (Ki)

dopamine D 2 receptor

5.9 nM (Ki)

P-Glycoprotein

体外研究

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.

体内研究

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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