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Submit ReviewNE 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.
NE 100 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 391.97 |
公式 | C23H33NO2.HCl |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 1.96 | 5 | |
DMSO | 39.2 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: NE 100 hydrochloride, NE 100 hydrochloride supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Sigma1, 3133, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NE 100 hydrochloride 的部分引用包括:
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
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平均评分: 3 (Based on 1 Review.)
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