产品说明书

Nizatidine

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Chemical Structure| 76963-41-2 同义名 : LY139037
CAS号 : 76963-41-2
货号 : A239574
分子式 : C12H21N5O2S2
纯度 : 98%
分子量 : 331.457
MDL号 : MFCD00865660
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
靶点

  • H2 receptor

    Histamine H2 receptor, IC50:0.9 nM
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].
临床研究
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 - -
实验方案
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
参考文献

[1]Ueki S, Seiki M, et al. Gastroprokinetic activity of nizatidine, a new H2-receptor antagonist, and its possible mechanism of action in dogs and rats. J Pharmacol Exp Ther. 1993 Jan;264(1):152-7.

[2]Lin TM, Evans DC, et al. Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. J Pharmacol Exp Ther. 1986 Nov;239(2):406-10.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Nizatidine. 2018 Jan 25

[4]Morton DM. Pharmacology and toxicology of nizatidine. Scand J Gastroenterol Suppl. 1987;136:1-8

[5]Futagami S, Shimpuku M, Song JM, Kodaka Y, Yamawaki H, Nagoya H, Shindo T, Kawagoe T, Horie A, Gudis K, Iwakiri K, Sakamoto C. Nizatidine improves clinical symptoms and gastric emptying in patients with functional dyspepsia accompanied by impaired gastric emptying. Digestion. 2012;86(2):114-21

[6]Ueki S, Matsunaga Y, Yoneta T, Tamaki H, Itoh Z. Gastroprokinetic activity of nizatidine during the digestive state in the dog and rat. Arzneimittelforschung. 1999 Jul;49(7):618-25