NE 100 hydrochloride
Potent and selective σ1 receptor antagonist (Ki = 0.86 nM) that displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. Exhibits reversible binding (Kd = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 391.97. Batch specific molecular weights may vary from batch to batch due to solvent 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||2.55 mL||12.76 mL||25.51 mL|
|5 mM||0.51 mL||2.55 mL||5.1 mL|
|10 mM||0.26 mL||1.28 mL||2.55 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the products' biological activity.
Chaki et al (1994) NE-100, a novel potent σ ligand, preferentially binds to σ1 binding sites in guinea pig brain. Eur.J.Pharmacol. 251 R1 PMID: 8137864
If you know of a relevant reference for NE 100 hydrochloride, please let us know.
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Keywords: NE 100 hydrochloride, supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience
3 Citations for NE 100 hydrochloride
Citations are publications that use Tocris products. Selected citations for NE 100 hydrochloride include:
Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Br J Pharmacol 6 35458 PMID: 26461475
Malik et al (2015) The effects of σ (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice. Int J Neuropsychopharmacol 172 2519 PMID: 25573298
Sánchez-Blázquez et al (2014) The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Eur J Immunol 17 1943 PMID: 24485144
Do you know of a great paper that uses NE 100 hydrochloride from Tocris? If so please let us know.
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