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尼扎替丁 /Nizatidine {[allProObj[0].p_purity_real_show]}

货号:A239574 同义名: LY139037 Ambeed 开学季,买赠积分,赢豪礼

Nizatidine is an antagonist of histamine H2 receptor that can inhibit the secretion of gastric acid.

Nizatidine 化学结构 CAS号:76963-41-2
Nizatidine 化学结构
CAS号:76963-41-2
Nizatidine 3D分子结构
CAS号:76963-41-2
Nizatidine 化学结构 CAS号:76963-41-2
Nizatidine 3D分子结构 CAS号:76963-41-2
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Nizatidine 纯度/质量文件 产品仅供科研

货号:A239574 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 {[allProObj[0].p_purity_real_show]}
Cyclizine {[allProObj[0].p_purity_real_show]}
Loratadine +

B(0)AT2, IC50: 4 μM

{[allProObj[0].p_purity_real_show]}
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

{[allProObj[0].p_purity_real_show]}
Doxylamine succinate {[allProObj[0].p_purity_real_show]}
Ebastine {[allProObj[0].p_purity_real_show]}
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

{[allProObj[0].p_purity_real_show]}
Meclizine dihydrochloride {[allProObj[0].p_purity_real_show]}
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
Diphenhydramine HCl {[allProObj[0].p_purity_real_show]}
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

{[allProObj[0].p_purity_real_show]}
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

{[allProObj[0].p_purity_real_show]}
Bilastine +++

H1 receptor, Ki: 44.15 nM

{[allProObj[0].p_purity_real_show]}
Pemirolast potassium {[allProObj[0].p_purity_real_show]}
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

{[allProObj[0].p_purity_real_show]}
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Brompheniramine maleate {[allProObj[0].p_purity_real_show]}
Carbinoxamine maleate salt {[allProObj[0].p_purity_real_show]}
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

{[allProObj[0].p_purity_real_show]}
Ketotifen fumarate salt {[allProObj[0].p_purity_real_show]}
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR {[allProObj[0].p_purity_real_show]}
Famotidine {[allProObj[0].p_purity_real_show]}
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

{[allProObj[0].p_purity_real_show]}
Lafutidine {[allProObj[0].p_purity_real_show]}
Cimetidine {[allProObj[0].p_purity_real_show]}
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE {[allProObj[0].p_purity_real_show]}
Ranitidine {[allProObj[0].p_purity_real_show]}
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

{[allProObj[0].p_purity_real_show]}
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

{[allProObj[0].p_purity_real_show]}
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

{[allProObj[0].p_purity_real_show]}
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

{[allProObj[0].p_purity_real_show]}
Azelastine HCl {[allProObj[0].p_purity_real_show]}
Epinastine HCl {[allProObj[0].p_purity_real_show]}
Levodropropizine {[allProObj[0].p_purity_real_show]}
Cyproheptadine hydrochloride {[allProObj[0].p_purity_real_show]}
Hesperetin {[allProObj[0].p_purity_real_show]}
Olopatadine HCl {[allProObj[0].p_purity_real_show]}
Mianserin hydrochloride {[allProObj[0].p_purity_real_show]}
Buclizine 2HCl {[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl GluR {[allProObj[0].p_purity_real_show]}
Cetirizine 2HCl {[allProObj[0].p_purity_real_show]}
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。

Nizatidine 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].

Nizatidine 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 - -

Nizatidine 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

Nizatidine 实验方案

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

Nizatidine 技术信息

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

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
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