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(Z)-Lafutidine

Names

[ CAS No. ]:
206449-93-6

[ Name ]:
(Z)-Lafutidine

[Synonym ]:
rac Lafutidine

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H29N3O4S

[ Molecular Weight ]:
431.54800

[ Exact Mass ]:
431.18800

[ PSA ]:
107.37000

[ LogP ]:
4.30450


Related Compounds