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尼普拉嗪 /Niaprazine {[allProObj[0].p_purity_real_show]}

货号:A156843

Niaprazine是一种组胺 H1 受体 (histamine H1-receptor) 拮抗剂,具有抗组胺和抗血清素活性,常用于睡眠障碍的研究,能够调控与神经传递相关的生理过程,适用于睡眠障碍及神经系统疾病的研究。

Niaprazine 化学结构 CAS号:27367-90-4
Niaprazine 化学结构
CAS号:27367-90-4
Niaprazine 3D分子结构
CAS号:27367-90-4
Niaprazine 化学结构 CAS号:27367-90-4
Niaprazine 3D分子结构 CAS号:27367-90-4
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Niaprazine 纯度/质量文件 产品仅供科研

货号:A156843 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Niaprazine 生物活性

描述 Niaprazine is a histamine H1 receptor antagonist. Niaprazine possesses antihistamine and antiserotonin activity and can be used in sleep disorder studies[1][2].Niaprazine has a low affinity for vesicular monoamine transporters as well as D2, α2, β, H1, and mAch receptors. Niaprazine, especially the (+) stereoisomer, has a high affinity for the α1 and 5-HT2 binding sites, with Ki's of 77 nM and 25 nM, respectively, but poorly recognises the 5-HT1A and 5-HT1B binding sites[2 ].

Niaprazine 动物研究

Animal study Niaprazine increases the concentration of 5-hydroxyindoleacetic acid (5-HIAA) in the rat brain 30 minutes after treatment and decreases it 3-8 hours after treatment when administered once intraperitoneally at a dose of 60 mg/kg. Niaprazine also transiently depletes norepinephrine (NA) and dopamine (DA) in the brain of the rat[3].

Niaprazine 参考文献

[1]D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001.

[2]P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50.

[3]P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

Niaprazine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL

Niaprazine 技术信息

CAS号27367-90-4
分子式C20H25FN4O
分子量 356.437
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(294.58 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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