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Submit ReviewPridopidine 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.
Pridopidine is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 281.42 |
Formula | C15H23NO2S |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 28.14 | 100 | |
ethanol | 28.14 | 100 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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
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Keywords: 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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