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Sazetidine A dihydrochloride

Cat. No. 2736 4 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： α4β2 nAChR ligand; may act as an agonist or a desensitizer
化学名： 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
纯度： ≥98% (HPLC)
说明书
引用文献 (4)
评论
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Sazetidine A dihydrochloride

Sazetidine A dihydrochloride is a subtype-selective α4β2 nicotinic acetylcholine receptor ligand (Ki values are 0.26 and 54 nM at α4β2 and α3β4 receptors respectively). May act as a silent desensitizer or as an agonist, depending on subunit stoichiometry (EC50 = 1.1 nM for nAChR-stimulated dopamine release). Exhibits analgesic activity in vivo and significantly reduces nicotine self-administration in an experimental rat model.

技术数据 for Sazetidine A dihydrochloride

分子量 333.25
公式 C15H20N2O2.2HCl
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2455450-63-0
PubChem ID 56972183
InChI Key WRSKKJWUXISFFU-UTLKBRERSA-N
Smiles OCCCCC#CC1=CN=CC(OC[C@H]2NCC2)=C1.Cl.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.

溶解性数据 for Sazetidine A dihydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 16.66 50

制备储备液 for Sazetidine A dihydrochloride

以下数据基于产品分子量 333.25。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.5 mM 6 mL 30.01 mL 60.02 mL
2.5 mM 1.2 mL 6 mL 12 mL
5 mM 0.6 mL 3 mL 6 mL
25 mM 0.12 mL 0.6 mL 1.2 mL

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产品说明书 for Sazetidine A dihydrochloride

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for Sazetidine A dihydrochloride

参考文献是支持产品生物活性的出版物。

Xiao et al (2006) Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 70 1454 PMID: 16857741

Cucchiaro et al (2008) Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 109 512 PMID: 18719450

Levin et al (2010) Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J.Pharmacol.Exp.Ther. 332 933 PMID: 20007754

Zwart et al (2008) Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol. 73 1843

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关键词: Sazetidine A dihydrochloride, Sazetidine A dihydrochloride supplier, α4β2, a4b2, receptor, ligands, agonists, desensitizers, desensitisers, Nicotinic, Receptors, Acetylcholine, nAChR, SazetidineA, dihydrochloride, 1197329-42-2, (a4b2), 2736, Tocris Bioscience

4 篇 Sazetidine A dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Sazetidine A dihydrochloride 的部分引用包括：

Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Nat Commun 8 e62246 PMID: 23638015

Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. PLoS One 40 2047 PMID: 24728867

Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396

Kiguchi (2018) Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. J Neuroinflammation 15 96 PMID: 29587798

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