Prevention by (R)-alpha-methylhistamine of ethanol-induced gastric mucosal lesions in rats: importance of adherent mucus gel layer.

G Morini, D Grandi, S Gentili, G Bertaccini
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Abstract

The ability of (R)-alpha-methylhistamine, the selective agonist of histamine H3 receptors, to reduce ethanol-induced gastric damage was examined in the rat. (R)-alpha-methylhistamine (1-100 mg/kg intragastrically) caused a dose-related reduction in the amount of damage produced by ethanol. This protective effect was not shared by the S enantiomer of alpha-methylhistamine. Thioperamide, selective H3 receptor antagonist, inhibited the protective effect of 10 but not 100 mg/kg of (R)-alpha-methylhistamine. Pretreatment with (R)-alpha-methylhistamine, 100 mg/kg i.g., resulted in a significant increase in the thickness of adherent mucus gel layer, which may contribute to the protective action of the compound.

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(R)- α -甲基组胺对乙醇诱导大鼠胃粘膜病变的预防作用:黏液凝胶层的重要性。
研究了组胺H3受体的选择性激动剂(R)- α -甲基组胺(R)- α -甲基组胺)减轻乙醇引起的大鼠胃损伤的能力。(R)- α -甲基组胺(1-100 mg/kg灌胃)导致乙醇产生的损伤量呈剂量相关减少。α -甲基组胺的S对映体没有这种保护作用。选择性H3受体拮抗剂硫哌丁胺能抑制10 mg/kg (R)- α -甲基组胺的保护作用,但不能抑制100 mg/kg的保护作用。(R)- α -甲基组胺预处理100 mg/kg ig后,粘附黏液凝胶层厚度显著增加,可能与化合物的保护作用有关。
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