Pridopidine

Pridopidine (FR310826) 是多巴胺稳定剂,是一种低亲和力的多巴胺 D2 受体拮抗剂。它高亲和力作用于 sigma 1受体,Ki=70-80 nM,比其对 D2R 的亲和力高约 100 倍。

CAS号

346688-38-8

分子式

C15H23NO2S

主要靶点

Dopamine Receptor

仅限科研使用

Cat No : CM06439

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Synonyms

ACR16|ASP2314|FR310826|4-[3-(甲磺酰基)苯基]-1-丙基哌啶



产品信息

Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist, improves motor performance and shows neuroprotective effects in Huntington disease R6/2 mouse model.

CAS号 346688-38-8
分子式 C15H23NO2S
主要靶点 Dopamine Receptor
主要通路 G蛋白偶联受体|神经科学
分子量 281.41
纯度 99.89%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 ACR16|ASP2314|FR310826|4-[3-(甲磺酰基)苯基]-1-丙基哌啶

靶点活性

sigma 1 receptor:70-80 nM (Ki)

体内活性

The actions of pridopidine were mediated by S1R and led to normalization of ER Ca2+ release, ER Ca2+ levels and spine SOC entry in YAC128 MSNs. This is a new potential mechanism of action for pridopidine, highlighting S1R as a potential target for HD therapy. Upregulation of striatal proteins that regulate calcium, including calbindin and homer1a, upon chronic therapy with pridopidine, may further contribute to long-term beneficial effects of pridopidine in HD[1].

溶解度

DMSO:50 mg/mL (177.68 mM)

动物实验

Sprague Dawley rats (n = 6) were treated daily by oral gavage with pridopidine (60 mg/kg) over 10 days. Six control Sprague Dawley rats were vehicle-treated. On the 10th day, 90 min following the last drug administration, brains were removed and RNA was isolated from the striatum of each rat and was analyzed using Affymetrix Rat 230_2 arrays. The gene expression data from 12 striatum samples was RMA normalized with affy package v1.42.3 in R v3.1.2. Probesets were annotated . The limma package v3.18.13 in R v3.1.3 was used to test if relevant calcium-related genes were differentially expressed between the two groups of biological replicates and multiple hypothesis testing was corrected for using the Bonferroni correction. Limma employs an empirical Bayes method to moderate standard error . When a gene had multiple probesets, the probeset with the highest absolute value of fold change was reported[1].

参考文献

1.Ryskamp D , Wu J , Geva M , et al. The sigma-1 receptor mediates the beneficial effects of pridopidine in a mouse model of Huntington disease[J]. Neurobiology of Disease, 2016, 97(Pt A):46-59.
2.Shannon, Kathleen M . Pridopidine for the treatment of Huntington’s disease[J]. Expert Opinion on Investigational Drugs, 2016:1-8.

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