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。
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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。 |
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 ]. |
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]. |
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 |
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 |