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Submit ReviewPridopidine
说明： Highly selective σ1 agonist
别名： PL-101,ACR16,Huntexil
化学名： 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine
纯度： ≥98% (HPLC)
生物活性 for Pridopidine
Pridopidine is a selective high affinity σ-1 receptor (S1R) agonist (Ki = 7.1 nM in both HEK293 cells and rat striatal membranes). Pridopidine displays ~30-fold and ~100-fold selectivity over the dopamine D3 receptor and the D2 receptor, respectively. Pridopidine is a low affinity dopamine D2 receptor antagonist (Ki (low) = 17.5 μM; Ki (high) = 7.5 μM). Pridopidine upregulates gene expression induced by BDNF in rat striatum in vivo in an S1R-dependent manner. Pridopidine improves motor function and shows neuroprotective effects in Huntington's disease animal models. Pridopidine restores neuromuscular junction activity in amyotrophic lateral sclerosis models in vitro and in vivo. Orally bioavailable.
化合物库 for Pridopidine
Pridopidine is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Pridopidine
| 分子量 | 281.42 |
| 公式 | C15H23NO2S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 346688-38-8 |
| PubChem ID | 9795739 |
| InChI Key | YGKUEOZJFIXDGI-UHFFFAOYSA-N |
| Smiles | CS(C1=CC(C2CCN(CCC)CC2)=CC=C1)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Pridopidine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 28.14 | 100 | |
| ethanol | 28.14 | 100 |
制备储备液 for Pridopidine
以下数据基于产品分子量 281.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.55 mL | 17.77 mL | 35.53 mL |
| 5 mM | 0.71 mL | 3.55 mL | 7.11 mL |
| 10 mM | 0.36 mL | 1.78 mL | 3.55 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.71 mL |
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产品说明书 for Pridopidine
参考文献 for Pridopidine
参考文献是支持产品生物活性的出版物。
Ionescu et al (2019) Targeting the sigma-1 receptor via pridopidine ameliorates central features of ALS pathology in a SOD1G93A model. Cell Death Dis. 10 210 PMID: 30824685
Geva et al (2016) Pridopidine activates neuroprotective pathways impaired in Huntington Disease. Hum.Mol.Genet. 25 3975 PMID: 27466197
Ye et al (2020) Small molecules selectively targeting sigma-1 receptor for the treatment of neurological diseases. J.Med.Chem. 63 15187 PMID: 33111525
Sahlholm et al (2013) The dopamine stabilizers ACR16 and (-)-OSU6162 display nanomolar affinities at the σ-1 receptor. Mol.Psychiatry 18 12 PMID: 22349783
Ryskamp et al (2017) The sigma-1 receptor mediates the beneficial effects of pridopidine in a mouse model of Huntington disease. Neurobiol.Dis. 97 46 PMID: 27818324
If you know of a relevant reference for Pridopidine, please let us know.
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关键词: Pridopidine, Pridopidine supplier, Selective, sigma, receptor, receptors, agonists, ligand, sigma1, ACR16, Huntexil, PL-101, high, affinity, dopamine, D2, antagonists, antagonism, Sigma1, Receptors, 7630, Tocris Bioscience
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