NE 100 hydrochloride

Cat. No. 3133

NE 100 hydrochloride C23H33NO2.HCl [149409-57-4]

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Chemical Name: 4-Methoxy-3-(2-phenylethoxy)-N,N-dipropylbenzeneethanamine hydrochloride

Biological Activity

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.

Technical Data

Soluble to 25 mM in water and to 100 mM in DMSO
>98 %
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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

If you know of a relevant reference for NE 100 hydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for NE 100 hydrochloride include:

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.

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.

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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Keywords: NE 100 hydrochloride, supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Tocris Bioscience, σ1 Receptor Antagonist products

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