A histamine H2 receptor antagonist with gastroprotective activity; inhibits histamine-induced cAMP production in CHO cells expressing human histamine H2 receptors at 10 nM; reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis at 3

Lafutidine – 250 mg

Brand:
Cayman
CAS:
118288-08-7
Storage:
-20
UN-No:
Non-Hazardous - /

Lafutidine is a histamine H2 receptor antagonist with gastroprotective activity.{53634} It inhibits histamine-induced cAMP production in CHO cells expressing human histamine H2 receptors when used at a concentration of 10 nM. Intragastric administration of lafutidine (3, 10, and 30 mg/kg) reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis.{53635} It prevents 5-fluorouracil-induced intestinal mucositis, diarrhea, and body weight loss in wild-type, but not Trpv1-/- or sensory deafferented, mice when administered at doses ranging from 3 to 30 mg/kg.{53636} Lafutidine (10 mg/kg) also reduces indomethacin-induced antral ulcer size in wild-type, but not chemically-deafferented, rats.{7826}  

 

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Description

A histamine H2 receptor antagonist with gastroprotective activity; inhibits histamine-induced cAMP production in CHO cells expressing human histamine H2 receptors at 10 nM; reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis at 3, 10, and 30 mg/kg; prevents 5-fluorouracil-induced intestinal mucositis, diarrhea, and body weight loss in wild-type, but not Trpv1-/- or sensory deafferented, mice from 3-30 mg/kg; reduces indomethacin-induced antral ulcer size in wild-type but not chemically-deafferented rats at 10 mg/kg

Formal name: (+)-2-[(2-furanylmethyl)sulfinyl]-N-[(2Z)-4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-buten-1-yl]-acetamide

Synonyms:  (+)-Lafutidine|FRG 8813

Molecular weight: 431.5

CAS: 118288-08-7

Purity: ≥98%

Formulation: A solid

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