Lafutidine

产品说明书

Print
Chemical Structure| 118288-08-7 同义名 : FRG-8813;(+)-Lafutidine
CAS号 : 118288-08-7
货号 : A101474
分子式 : C22H29N3O4S
纯度 : 99%
分子量 : 431.548
MDL号 : MFCD21607521
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(115.86 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
动物实验配方：
生物活性
靶点

  • H2 receptor
描述 Lafutidine, a histamine H2 receptor antagonist with mucosal protective properties via sensory afferent neurons, is used for the treatment of upper gastrointestinal diseases. Daily administration of lafutidine reduced the severity of intestinal mucositis, diarrhea and body weight loss in a dose-dependent manner. Lafutidine attenuates 5-FU-induced intestinal mucositis, most likely by increasing mucus production via activation of sensory afferent neurons[3]. Lafutidine exhibited potent and long-lasting H2 antagonism and prolonged antisecretion. Lafutidine showed antiulcer activities against acute ulcer models, prevented gastric ulcer relapse of acetic ulcer, and accelerated the healing of indomethacin-induced antral ulcers in rats[4]. Intracisternal injection of RX 77368 (1.5 ng) or intraportal lafutidine (10 mg/kg) by itself did not affect hepatic blood flow, but co-injection of intracisternal RX 77368 (1.5 ng) and intraportal lafutidine (5 mg/kg) increased it with peak response at 30 min postinjection. The effect of lafutidine on hepatic blood flow in rats given RX 77368 was dose-related over the range 1 - 5 mg/kg[5]. Lafutidine, however, was superior to famotidine in terms of symptom relief of reflux esophagitis[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
NCT02703896 Pulmonary Aspiration of Gastri... 展开 >>c Contents 收起 << Phase 4 Completed - -
NCT02555852 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT00229424 Gastroesophageal Reflux Phase 3 Completed - Japan ... 展开 >> Tohoku University Hospital 1-1, Seiryo-cho, Aoba-ku, Sendai, Miyagi, Japan, 980-8574 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.17mL

4.63mL

2.32mL
参考文献

[1]Namikawa T, Munekage E, et al. Feasibility study of supportive care using lafutidine, a histamine H2 receptor antagonist, to prevent gastrointestinal toxicity during chemotherapy for gastric cancer. Anticancer Res. 2014 Dec;34(12):7297-301.

[2]Tanaka M, Banba M, et al. Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86.

[3]Sano T, Utsumi D, Amagase K, Matsumoto K, Tominaga M, Higuchi K, Takeuchi T, Kato S. Lafutidine, a histamine H2 receptor antagonist with mucosal protective properties, attenuates 5-fluorouracil-induced intestinal mucositis in mice through activation of extrinsic primary afferent neurons. J Physiol Pharmacol. 2017 Feb;68(1):79-90

[4]Tanaka M, Banba M, Joko A, Moriyama Y. [Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86. Japanese

[5]Yoneda M, Kurosawa M, Watanobe H, Terano A. Lafutidine increases hepatic blood flow via potentiating the action of central thyrotropin-releasing hormone in rats. J Gastroenterol Hepatol. 2003 Feb;18(2):177-84

[6]Kim EH, Lee YC, Chang YW, Park JJ, Chun HJ, Jung HY, Kim HS, Jeong HY, Seol SY, Han SW, Choi MG, Park SH, Lee OJ, Jung JT, Lee DH, Jung HC, Lee ST, Kim JG, Youn SJ, Kim HY, Lee SW. Efficacy of Lafutidine Versus Famotidine in Patients with Reflux Esophagitis: A Multi-Center, Randomized, Double-Blind, Non-inferiority Phase III Trial. Dig Dis Sci. 2015 Jun;60(6):1724-32