Lafutidine_product_DataBase

Bioactivity

Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease[1].

Target

Histamine H2-receptor

Invitro

Lafutidine exhibits gastric mucosal protective action mediated by capsaicin-sensitive afferent neurons, in addition to a potent antisecretory effect[2].Lafutidine (0.1-10 µM) significantly augments the periarterial nerve stimulation (PNS, 1 Hz) induced-vasodilation in a concentration-dependent manner in rat perfused mesenteric vascular beds[2].

In Vivo

Lafutidine (3-30 mg/kg; p.o.; twice daily; for 6 days) dose-dependently reduces the severity of dextran sulfate Na (DSS)-induced colitis and significantly mitigates changes in the colon length and myeloperoxidase (MPO) activity[3]. Animal Model:

Name

Lafutidine

CAS

118288-08-7

Formula

C22H29N3O4S

Molar Mass

431.55

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Motoko Nakano, et al. Possible involvement of host defense mechanism in the suppression of rat acute reflux esophagitis by the particular histamine H2 receptor antagonist lafutidine. Pharmacology. 2012;90(3-4):205-11. [2]. Tetsuhiro Sugiyama, et al. Lafutidine facilitates calcitonin gene-related peptide (CGRP) nerve-mediated vasodilation via vanilloid-1 receptors in rat mesenteric resistance arteries. J Pharmacol Sci. 2008 Mar;106(3):505-11. [3]. Mitsuaki Okayama, et al. Protective effect of lafutidine, a novel histamine H2-receptor antagonist, on dextran sulfate sodium-induced colonic inflammation through capsaicin-sensitive afferent neurons in rats. Dig Dis Sci. 2004 Oct;49(10):1696-704.

PeptideDB

Lafutidine

CAS: 118288-08-7 F: C22H29N3O4S W: 431.55