溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
产品介绍 | Cariprazine(RGH188)有抗精神病活性,对D3和D2受体有较高亲和力,Ki分别为0.09 nM和0.5 nM,对5-HT(1A)受体有一定亲和力。 |
生化机理 | Description:IC50 Value: 0.5 and 0.09 nM (Ki for D2 and D3 receptor respectively); 2.6 and 180 nM(Ki for 5-HT1A and 5-HT2A receptor respectively) [1]Cariprazine is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D(3) and D(2) receptors and moderate affinity to serotonin 5-HT(1A) receptors.in vitro: Cariprazine had lower affinity at human and rat hippocampal 5-HT(1A) receptors (pK(i) 8.59 and 8.34, respectively) and demonstrated low intrinsic efficacy.Cariprazine displayed low affinity at human 5-HT(2A) receptors (pK(i) 7.73). Moderate or low affinity for histamine H(1) and 5-HT(2C) receptors (pK(i) 7.63 and 6.87, respectively) suggest cariprazine's reduced propensity for adverse events related to these receptors [2].in vivo: Doses ≥ 1.5 mg/d yielded 69 - 75% D2/D3 receptor occupancy as measured in positron emission tomography scans. Mean half-life for cariprazine was 2 - 5 d over a dose ra |
别名 | 卡利拉嗪;RGH-188;RGH 188;RGH188;n'-(trans-4-(2-(4-(2,3-dichlorophenyl)-1-piperazinyl)ethyl)cyclohexyl)-n,n-dimethylurea |
卡利拉嗪
Cariprazine (订货以英文为准)
编号:C126186
CAS号:839712-12-8
分子式:C21H32CL2N4O
分子量:427.41
产品名称 | Cariprazine |
中文名称 | 卡利拉嗪 |
CAS号 | 839712-12-8 |
分子式(M.F.) | C21H32CL2N4O |
分子量(M.W.) | 427.41 |
储存条件 | -20°C储存 |
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