计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Pridopidine 是一种多巴胺 (DA) 稳定剂，可用作一种低亲和力的多巴胺 D2 受体 (D2R) 拮抗剂。Pridopidine 高亲和力作用于 sigma 1受体 (S1R)，Ki 值为 70 到 80 nM，比其对 D2R 的亲和力高约 100 倍。
Pridopidine, a dopamine ( DA ) stabilizer, acts as a low affinity dopamine D2 receptor ( D2R ) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor ( S1R ) with K i between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
In Vitro
Pridopidine, a dopamine (DA) stabilizer, Pridopidine may be a neuromodulatory agent with neuroprotective properties in Huntington disease (HD). To clarify the neuroprotective efficacy of Pridopidine and to explore the potential underling molecular mechanism, the ability of Pridopidine is evaluated to protect cells from apoptosis and to eventually activate pro-survival targets. Administration of Pridopidine (150 μM), the most effective dose, significantly reduces apoptosis in immortalized striatal knock-in cells expressing endogenous levels of mutant Htt (STHdh 111/111 ) and markedly enhances phosphorylation state of prosurvival kinase ERK. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pridopidine is known to act as a low affinity D2R antagonist. Pridopidine’s activity may be attributed to binding the sigma 1 receptor (S1R), an endoplasmic reticulum (ER). To strengthen the hypothesis that the BDNF pathway is upregulated due to activation of the S1R, SD rats are treated with lower doses of Pridopidine (range 0.3-60 mg/kg), and analysed the expression of seven selected genes in the BDNF pathway by qPCR. Pridopidine doses of 3 and 15 mg/kg in rats occupy 57±2% and 85±2% of S1R, respectively, and both do not show occupancy of the D2R, as determined by in vivo PET imaging. The significant occupancy proportion of the D2R (44-66%) is observed only at a dose of 60 mg/kg. This PET study supports the conclusion that the upregulation of genes in rats treated with 15 mg/kg Pridopidine are a result of specific activation of the S1R. At 30 mg/kg, partial/low occupancy of the D2R is at levels of 22-33% (assuming linearity), and S1R is saturated. Indeed, qPCR analysis reveals that the upregulation of EGR1 (already up at 3 mg/kg), EGR2, HOMER1A, KLF5, and ARC expression are upregulated at the low 15 mg/kg dose and expression of CDNK1A and CEBPB are significantly upregulated from a low dose of 30 mg/kg (CEBPB is significantly increased at 3 mg/kg but not at 15 mg/kg) . To further confirm the beneficial effect of Pridopidine on HD motor phenotype and to elucidate whether Pridopidine may act also as neuroprotective agent, preclinical studies in R6/2 mice have been undertaken. Daily administration of Pridopidine at a dose of 5 mg/kg, the most effective dose with no adverse effects, starting at the pre-symptomatic stage at 5 weeks for 6 weeks, significantly preserves motor function and prevents the progressive and dramatic motor worsening commonly observed in R6/2 mice. The beneficial effects of Pridopidine are maintained for about 4 weeks, after which mice show a slight worsening in performing both the horizontal ladder task and the open field. In addition, according to a Kaplan-Meier survival curve analysis, Pridopidine efficiently extends lifespan in the same mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
Conditionally immortalized mouse striatal knock-in cells expressing endogenous levels of wild-type (STHdh 7/7 ) or mHtt (STHdh 111/111 ) are used. Different concentrations of Pridopidine (100, 150, 200 and 300 μM) are tested to investigate the anti-apoptotic effect of the molecule on immortalized cells cultured in serum-free medium at 39°C for six hours. In NE100 experiments, cells are pre-incubated with the compound (10 μM) for 2 hrs before culturing them in apoptotic conditions. At the end of each treatment, cells are collected and incubated with FITC-conjugated Annexin V. Fluorescence Activated Cell Sorting (FACS) analysis is performed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:D 2 Receptor
规格
别名
普利多比定
规格或纯度
10mM in DMSO
英文名称
Pridopidine
生化机理
普利多哌啶是一种多巴胺（DA）稳定剂，是一种低亲和力的多巴胺 D2 受体（D2R）拮抗剂。普利多哌啶对 sigma 1 受体（S1R）具有高亲和力，K i 在 70 至 80 nM 之间，比其对 D2R 的亲和力高出约 100 倍。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
调节剂
作用机制
多巴胺 D2 受体调节剂
名称和识别符
EC号
810-806-1
分子类型
小分子
Isomeric SMILES
CCCN1CCC(CC1)C2=CC(=CC=C2)S(=O)(=O)C
PubChem CID
分子量
281.41
技术文档
高级数据
产品属性
| ALogP | 2.6 |
|---|
关联靶点（人）
SIGMAR1
Tclin
Sigma 非阿片类细胞内受体 1(Sigma non-opioid intracellular receptor 1)
(1 活性数据)
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 346688-38-8，分子式为 C15H23NO2S，分子量为 281.41 g/mol。
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