Nisoxetine
目录号: PL07516 纯度: ≥98%
CAS No. :53179-07-0
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中文名称
Nisoxetine
中文别名
尼索西汀
英文名称
Nisoxetine
英文别名
Benzenepropanamine, g-(2-methoxyphenoxy)-N-methyl-;3-(2-Methoxyphenoxy)-N-methyl-3-phenyl-1-propanamine;[3H]-Nifedipine;[3H]-Nisoxetine;1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine-dicarboxylic acid dimethyl ester;4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine;4-(2-nitrophenyl)-3,5-dimethoxycarbonyl-2,6-dimethyl-1,4-dihydropyridine;Adalat;Corinfar;Fenihidin;Fenihidine;nifedipine;N-methyl-3-(2-methoxyphenoxy)-3-phenyl-1-propylamine;N-methyl-3-(2-methoxyphenoxy)-3-phenylpropylamine;Procardia;Nisoxetine
Cas No.
53179-07-0
分子式
C17H21NO2
分子量
271.35
包装储存
Pure form -20°C 3 years;4°C 2 years
产品详情
Nisoxetine 是一种有效的和选择性的去甲肾上腺素转运蛋白 (NET) 抑制剂,Kd 值为 0.76 nM。Nisoxetine 是一种抗抑郁试剂和局部麻药,它可以阻断电压门控性钠通道。
生物活性
Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a K d of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
性状
Viscous liquid
IC50 & Target[1][2]
Kd: 0.76 nM (NET)
体外研究(In Vitro)
Nisoxetine 抑制 [H]Nisoxetine 与大鼠额叶皮层膜的结合,Ki 为 1.4±0.1 nM。
Nisoxetine 抑制[H]去甲肾上腺素摄取到大鼠额叶皮质突触体中,Ki 为 2.1±0.3 nM。
Nisoxetine 抑制 Na 电流,膜电位为 -70 和 -100 mV 时的 IC50 分别为 1.6 和 28.6 μM。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Nisoxetine (2.2 μM; a single intrathecal injection) shows 100, 100, and 100% of blockades in motor function, proprioception, and with duration of action of about 61, 96, and 236 min, respectively.
Nisoxetine (3,10, 30 mg/kg, i.p.) inhibits refeeding response (intake of standard chow) in rats.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[1]. Bé?que JC, et, al. Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters. Eur J Pharmacol. 1998 May 15; 349(1): 129-32.
[2]. Cheetham SC, et, al. [3H]nisoxetine-a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan; 35(1): 63-70.
溶解度数据
In Vitro: DMSO : 250 mg/mL (921.32 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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