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  • Cariprazine hydrochloride
    • 盐酸卡利拉嗪;卡利拉嗪盐酸盐
    货号: abs813094
    CAS号: 1083076-69-0
    分子式: C21H33Cl3N4O
    分子量: 463.872
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    货号-规格 货期 价格 数量
    abs813094-5mg 1-2周 ¥1433.00
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    abs813094-10mg 1-2周 ¥2536.00
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    abs813094-50mg 1-2周 ¥7718.00
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    大包装询价
    产品描述
    描述

    Cariprazine(RGH188)盐酸盐有抗精神病活性,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。

    纯度
    98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    盐酸卡利拉嗪;卡利拉嗪盐酸盐
    可溶性/溶解性
    10 mM in DMSO
    生物活性
    靶点
    5-HT Receptor
    In vitro(体外研究)
    Cariprazine stimulates inositol phosphate (IP) formation with a high potency (pEC50 8.5) with relatively low efficacy (Emax 30%). Cariprazine, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D3 versus human D2L and human D2S receptors (pKi 10.07, 9.16, and 9.31, respectively). Cariprazine displays high affinity at human serotonin (5-HT) type 2B receptors (pKi 9.24) with pure antagonism. Cariprazine has lower affinity at human and rat hippocampal 5-HT1A receptors (pKi 8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Cariprazine displays low affinity at human 5-HT2A receptors (pKi 7.73). Moderate or low affinity for histamine H1 and 5-HT2C receptors (pKi 7.63 and 6.87, respectively) suggest Cariprazine's reduced propensity for adverse events related to these receptors. Cariprazine is over sixfold more potent (EC50=1.4 nM) than Aripiprazole (EC50=9.2 nM) in inhibiting isoproterenol-induced cAMP production in HEK-293 cells.
    In vivo(体内研究)
    Administration of Cariprazine (30 µg/kg) reduces the striatal uptake of both radioligands to the level of nonspecific binding compared with baseline PET measurements. Cariprazine has negligible effect on the time-activity curves in the cerebellum. At doses of 5.0 and 30 µg/kg, Cariprazine causes a dose-dependent dopamine D2/D3 receptor occupancy of ~45% and ~80% for both antagonist raclopride and agonist radioligand MNPA. Receptor occupancy of dopamine D2/D3 receptors calculated using the transient equilibrium and the MRTM2 methods ranged from 5% at the lowest dose (1.0 µg/kg) to 94% at the highest dose (300 µg/kg). The effects of 5 doses of Cariprazine (ranging from 0.005 to 0.15 mg/kg) are examined on EPM behavior of wild-type mice. Whereas lower doses of Cariprazine (0.005 to 0.02 mg/kg) do not alter the time spent in open arms, the two higher doses (0.08 and 0.15 mg/kg) lead to a significant decline of this measure (ANOVA, (F(5,52)=4.20; p=0.0032)). Moreover, the two higher doses of Cariprazine also lead to a significant decrease in the total number of arm entries (F(5,52)=7.21; p=0.0001)) but this decrease in the total number of arm entries is largely accounted for by a significant decrease in the number of closed arm entries (F(5,52)=11.75; p=0.0001)). The two highest doses of Cariprazine (0.08 and 0.15 mg/kg) have significant effects on locomotor activity, but doses ranging from 0.005 to 0.02 mg/kg do not affect anxiety-like behavior or locomotor activity in the EPM test. A significant (P.
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