Poli E, Stark H, Bertaccini G
Institute of Pharmacology, University of Parma, Ospedale Maggiore, Italy.
Agents Actions. 1991 May;33(1-2):167-9. doi: 10.1007/BF01993157.
The role of histamine H3-receptors in the control of acetylcholine release from peripheral cholinergic neurons was evaluated in the isolated guinea pig ileum, previously loaded with 3H-choline. When tested in the presence of H1- and H2-blockade, histamine (0.1-100 mumol/l) and (R) alpha-methylhistamine (0.01-1 mumol/l) dose-dependently reduced the electrically-evoked choline outflow, with (R) alpha-methylhistamine being a partial agonist. Selective H3-receptor blocking drugs, thioperamide (0.1 mumol/l) and impromidine (0.1 mumol/l) reversed the histamine-induced inhibitory effect. These data suggest that intestinal cholinergic nerves are endowed with histamine H3-receptors whose activation produces an inhibitory effect upon acetylcholine release. The practical implications of these findings are obvious.
在预先装载了3H-胆碱的离体豚鼠回肠中，评估了组胺H3受体在控制外周胆碱能神经元乙酰胆碱释放中的作用。在H1和H2受体阻断存在的情况下进行测试时，组胺（0.1 - 100 μmol/L）和（R）α-甲基组胺（0.01 - 1 μmol/L）剂量依赖性地减少电诱发的胆碱流出，（R）α-甲基组胺为部分激动剂。选择性H3受体阻断药物硫丙酰胺（0.1 μmol/L）和英普咪定（0.1 μmol/L）可逆转组胺诱导的抑制作用。这些数据表明，肠道胆碱能神经具有组胺H3受体，其激活对乙酰胆碱释放产生抑制作用。这些发现的实际意义是显而易见的。
