Lafutidine

SKU: orb1226861

Description

Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.(In Vitro):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.(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 118288-08-7
• MW: 431.55
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₉N₃O₄S
• SMILES: C1CCN(CC1)CC2=CC(=NC=C2)OC/C=C\CNC(=O)CS(=O)CC3=CC=CO3
• Target: 5-HT Receptor
• Solubility: Ethanol: 13 mg/mL (30.12 mM); DMSO: 86 mg/mL (199.28 mM)

Bioactivity

• 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. Animal model: Male Wistar rats (180-200 g). Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg. Administration: Oral administration, twice daily, for 6 days. Result: Reduced the severity of DSS-induced ulcerative colitis in a dose-dependent manner.
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• In Vitro:
  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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor