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NE 100 hydrochloride
Biological Activity for NE 100 hydrochloride
NE 100 hydrochloride is a 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.
Compound Libraries for NE 100 hydrochloride
Technical Data for NE 100 hydrochloride
|Storage||Store at -20°C|
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.
Solubility Data for NE 100 hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for NE 100 hydrochloride
The following data is based on the product molecular weight 391.97. 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||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|
Product Datasheets for NE 100 hydrochloride
References for NE 100 hydrochloride
References are publications that support the biological activity of the product.
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
Okuyama et al (1993) NE-100, a novel sigma receptor ligand: in vivo tests. Pharmacol.Letts. 53 PL285
Tanaka et al (1995) Characteristics of binding of [3H]NE-100, a novel sigma-receptor ligand, to guinea-pig brain membranes. Naunyn Schmied.Arch.Pharmacol. 351 244
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Keywords: NE 100 hydrochloride, NE 100 hydrochloride supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Sigma1, 3133, Tocris Bioscience
6 Citations for NE 100 hydrochloride
Citations are publications that use Tocris products. Selected citations for NE 100 hydrochloride include:
Atzmon et al (2018) Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy. Front Mol Neurosci 11 336 PMID: 30279648
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
Maurice (2017) Amyloid toxicity is enhanced after pharmacological or genetic invalidation of the σ1 receptor. Behav Brain Res 339 1 PMID: 29129596
Fishback et al (2012) A 96-well filtration method for radioligand binding analysis of σ receptor ligands. J Pharm Biomed Anal 71 157 PMID: 22910107
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? Please let us know.
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