Nizatidine is an antagonist of histamine H2 receptor that can inhibit the secretion of gastric acid.
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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 |
++
rat H3 receptor, Ki: 1.44 μM human H3 receptor, Ki: 1.2 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。 |
靶点 |
|
描述 | Nizatidine is a histamine type 2 receptor antagonist (H2 blocker) which is widely used for treatment of acid-peptic disease and heartburn. Nizatidine has been linked to rare instances of clinically apparent acute liver injury[3]. In rat and dog models, species in which the absorption, plasma half-life and routes of metabolism are similar to that of humans, nizatidine was three- to four-fold more active than cimetidine and was of similar potency to ranitidine. Nizatidine was well-tolerated in animals after both intravenous and oral administration and following single or repeated administration[4]. Nizatidine administration significantly improved both gastric emptying and clinical symptoms in FD (functional dyspepsia) patients with impaired gastric emptying[5]. Intravenous administration of nizatidine (0.3 - 3 mg/kg) enhanced the motility of the gastric antrum and duodenum during the digestive state. Gastric emptying of a solid test meal was accelerated by intraperitoneal administration of nizatidine (1 - 10 mg/kg) to the same extent as cisapride (0.1 - 1 mg/kg). Furthermore, nizatidine improved clonidine-induced delayed gastric emptying[6]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03509831 | Gastritis | Phase 1 | Active, not recruiting | April 2018 | Korea, Republic of ... 展开 >> Kukje Pharm Seongnam-si, Korea, Republic of 收起 << |
NCT02555852 | - | Completed | - | Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 << | |
NCT02703896 | Pulmonary Aspiration of Gastri... 展开 >>c Contents 收起 << | Phase 4 | Completed | - | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.02mL 0.60mL 0.30mL |
15.08mL 3.02mL 1.51mL |
30.17mL 6.03mL 3.02mL |
CAS号 | 76963-41-2 |
分子式 | C12H21N5O2S2 |
分子量 | 331.457 |
别名 | LY139037 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 50 mg/mL(150.85 mM),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 H2O: 20 mg/mL(60.34 mM),配合低频超声助溶 |
动物实验配方 |