206449-93-6

206449-93-6 structure

Name: (Z)-Lafutidine
Chemical Name: 2-(furan-2-ylmethylsulfinyl)-N-[4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide
CAS Number: 206449-93-6
Molecular Formula: C₂₂H₂₉N₃O₄S
Molecular Weight: 431.54800
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-06-19 22:20:48
Modify Date: 2024-01-10 17:45:50
(Z)-Lafutidine ((Z)-FRG-8813) is a potent histamine H2 receptor antagonist. (Z)-Lafutidine shows anti-secretory and gastroprotective activities[1].

Name	2-(furan-2-ylmethylsulfinyl)-N-[4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide
Synonyms	rac Lafutidine

Description	(Z)-Lafutidine ((Z)-FRG-8813) is a potent histamine H2 receptor antagonist. (Z)-Lafutidine shows anti-secretory and gastroprotective activities[1].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
In Vivo	(Z)-Lafutidine (Compound 16) stimulates mucin biosynthesis in rat gastric mucosa and this effect not directly due to histamine H2 receptor antagonism[1]. Animal Model: Eight- to nine-week-old male C57BL/6 mice weighing 20-24g[1] Dosage: 3-30 mg/kg Administration: P.o; twice for 6 days (5-FU: 50 mg/kg; i.p.;once daily) Result: Reduced the severity of diarrhea during 5-FU treatment,in a mostly dose-dependent manner, and a significant effect was observed at a dose of 30 mg/kg.
References	[1]. Hirakawa N, et al. A novel histamine 2(H2) receptor antagonist with gastroprotective activity. II. Synthesis and pharmacological evaluation of 2-furfuryl-thio and 2-furfurylsulfinyl acetamide derivatives with heteroaromatic rings. Chem Pharm Bull (Tokyo). 1998;46(4):616-622.