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Cariprazine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cariprazine图片
CAS NO:839712-12-8
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
卡利拉嗪
RGH-188
产品介绍
Cariprazine是一种新型抗精神病候选药物,结合D3,D25-HT1AKi为0.085 nM,0.49 nM,2.6 nM。
生物活性

Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for theD3(Ki=0.085 nM) andD2(Ki=0.49 nM) receptors, and moderate affinity for the5-HT1Areceptor (Ki=2.6 nM).

IC50& Target

D2Receptor

0.49 nM (Ki)

D3Receptor

0.085 nM (Ki)

5-HT1AReceptor

2.6 nM (Ki)

体外研究
(In Vitro)

Cariprazine stimulates inositol phosphate (IP) formation with a high potency (pEC508.5) with relatively low efficacy (Emax30%)[2]. Cariprazine, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D3versus human D2Land human D2Sreceptors (pKi10.07, 9.16, and 9.31, respectively). Cariprazine displays high affinity at human serotonin (5-HT) type 2B receptors (pKi9.24) with pure antagonism. Cariprazine has lower affinity at human and rat hippocampal 5-HT1Areceptors (pKi8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Cariprazine displays low affinity at human 5-HT2Areceptors (pKi7.73). Moderate or low affinity for histamine H1and 5-HT2Creceptors (pKi7.63 and 6.87, respectively) suggest Cariprazine's reduced propensity for adverse events related to these receptors[2]. 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[4].

体内研究
(In Vivo)

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/D3receptor occupancy of ~45% and ~80% for both antagonist [11C] raclopride and agonist radioligand [11C]MNPA. Receptor occupancy of dopamine D2/D3receptors 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)[1]. 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[3]. A significant (P<0.01) reduction in ouabain-induced hyperactivity is observed after acute i.p. administration of all doses of Cariprazine (mean±SEM: 0.06 mg/kg, 64.2±3.88; 0.25 mg/kg, 72.7±11.67; 0.5 mg/kg, 40.6±5.32; 1 mg/kg, 19.5±8.78) and lithium (40.4±12.78), compared with ouabain injection alone (114.6±14.33). The highest Cariprazine dose produced significant sedation (72% inhibition for Cariprazine 1.0 mg/kg aCSF vs. saline aCSF; P<0.05)[4].

Clinical Trial
分子量

427.41

性状

Solid

Formula

C21H32Cl2N4O

CAS 号

839712-12-8

中文名称

卡利拉嗪

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 2 mg/mL(4.68 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3397 mL11.6984 mL23.3967 mL
5 mM---------
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。