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Submit ReviewNE 100 hydrochloride
Description: Selective σ1 antagonist
Chemical Name: 4-Methoxy-3-(2-phenylethoxy)-N,N-dipropylbenzeneethanamine hydrochloride
Purity: ≥98% (HPLC)
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
NE 100 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for NE 100 hydrochloride
| M. Wt | 391.97 |
| Formula | C23H33NO2.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 149409-57-4 |
| PubChem ID | 9952420 |
| InChI Key | ZHGMDXSHODHWHV-UHFFFAOYSA-N |
| Smiles | CCCN(CCC)CCC1=CC=C(OC)C(OCCC2=CC=CC=C2)=C1.Cl |
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 | |
|---|---|---|---|
| Solubility | |||
| water | 1.96 | 5 | |
| DMSO | 39.2 | 100 |
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 |
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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
If you know of a relevant reference for NE 100 hydrochloride, please let us know.
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Keywords: NE 100 hydrochloride, NE 100 hydrochloride supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Sigma1, 3133, Tocris Bioscience
8 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
Song et al (2022) Sigma non-opioid receptor 1 is a potential therapeutic target for long QT syndrome. Nat.Card.Res. 1 142 PMID: 36051854
Morató et al (2023) Development of a novel σ1 receptor biosensor based on its heterodimerization with binding immunoglobulin protein in living cells. ACS Chem.Neurosci. PMID: 37191585
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
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
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
Maurice (2017) Amyloid toxicity is enhanced after pharmacological or genetic invalidation of the σ1 receptor. Behav Brain Res 339 1 PMID: 29129596
Do you know of a great paper that uses NE 100 hydrochloride from Tocris? Please let us know.
Reviews for NE 100 hydrochloride
Average Rating: 3 (Based on 1 Review.)
Have you used NE 100 hydrochloride?
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It can inhibit sigma1 receptor.
By
Yuyang Sun on 06/29/2022
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: sh-sy5y
Used it to inhibit sigma 1 receptors. It can inhibit sigma 1 receptor and increase SOCE channels.
