Comparison of the protective effect of (R)-alpha-methylhistamine and its prodrugs on gastric mucosal damage induced by ethanol in the rat.
1. The gastroprotective activity of two azomethine prodrugs of (R)-alpha-methylhistamine was examined in lesions induced by absolute ethanol (1 ml/rat intragastrically for 1 h). 2. Pretreatment with (R)-alpha-methylhistamine as well as with the prodrugs (30 and 100 mg/kg intragastrically [IG]) significantly reduced macroscopically visible lesions caused by ethanol, with protection being almost complete at 100 mg/kg. 3. Histologically, in rats pretreated with the three compounds at a dose of 100 mg/kg, the evidence of damage was rare, with the appearance of gastric mucosa being similar in the different groups. 4. Present results are suggestive of a local component in the protective activity of (R)-alpha-methylhistamine.
Morini
G
G
Institute of Pharmacology, University of Parma, Italy.
Grandi
D
D
Bertaccini
G
G
D000818:Animals; D000431:Ethanol / Q000009:adverse effects*; D005753:Gastric Mucosa / Q000187:drug effects* / Q000473:pathology; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control; D017442:Histamine Agonists / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D008761:Methylhistamines / Q000494:pharmacology / Q000627:therapeutic use*; D009336:Necrosis; D011355:Prodrugs / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar
D017442:Histamine Agonists; D008761:Methylhistamines; D011355:Prodrugs; D000431:Ethanol; C069357:alpha-methylhistamine