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Cariprazine hydrochloride (RGH188 hydrochloride) 是一种抗精神病药物,是一种 D3 和 D2 受体部分激动剂,Ki 分别为 0.09 nM 和 0.5 nM,对5-HT(1A)受体有一定亲和力。
Cariprazine hydrochloride (RGH188 hydrochloride) 是一种抗精神病药物,是一种 D3 和 D2 受体部分激动剂,Ki 分别为 0.09 nM 和 0.5 nM,对5-HT(1A)受体有一定亲和力。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 239 | 现货 | |
10 mg | ¥ 389 | 现货 | |
25 mg | ¥ 622 | 现货 | |
50 mg | ¥ 970 | 现货 | |
100 mg | ¥ 1,470 | 现货 | |
500 mg | ¥ 3,670 | 现货 |
产品描述 | Cariprazine hydrochloride (RGH188 hydrochloride) is an antipsychotic drug, is a D3 and D2 receptor partial agonist((Ki of 0.085 nM and 0.49 nM, respectively) |
靶点活性 | D2 receptor:0.49 nM (Ki) , 5-HT1A receptor:2.6 nM (Ki), D3 receptor:0.085 nM (Ki) |
体内活性 | Cariprazine以剂量依赖和可饱和的方式占据D(2)/D(3)受体,最低剂量占据约5%的受体,而最高剂量显示出超过90%的占据率。与同等剂量的D(2)/D(3)占据相比,5-HT(1A)受体的占据率显著较低,其在raphe nuclei[1]的最大值约为30%。 |
动物实验 | Three monkeys using the following PET radioligands: [(11)C]MNPA (an agonist at D(2) and D(3) receptors), [(11)C]raclopride (an antagonist at D(2) and D(3) receptors), and [(11)C]WAY-100635 (an antagonist at 5-HT(1A) receptors). During each experimental day, the first PET measurement was a baseline study, the second after a low dose of cariprazine, and the third after the administration of a high dose[1]. |
别名 | Cariprazine HCl, 盐酸卡利拉嗪, RGH188 hydrochloride |
分子量 | 463.87 |
分子式 | C21H33Cl3N4O |
CAS No. | 1083076-69-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: < 1 mg/mL (insoluble), Sonication is recommended. |
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