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Lafutidine (FRG-8813) is a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion. Lafutidine exhibits gastric mucosal protective action mediated by capsaicin-sensitive afferent neurons, in addition to a potent antisecretory effect. 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. 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.
| Molecular Weight | 431.55 |
| Formula | C22H29N3O4S |
| CAS Number | 118288-08-7 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histamine Receptor Products |
|---|
| Ciproxifan maleate
Ciproxifan is an orally bioavailable, extremely potent histamine H3 inverse agonist/antagonist. |
| Antazoline hydrochloride
Antazoline hydrochloride is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. |
| Azacyclonol
Azacyclonol, also known as γ-pipradol, which diminishes hallucinations in psychotic individuals. |
| Azatadine dimaleate
Azatadine dimaleate is an antihistamine and anticholinergic compound with IC50 of 6.5nM and 10nM, respectively. |
| Bepotastine Besilate
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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