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Effects of 3-methylhistamine and phenylethylamine on histamine action on isolated guinea-pig trachea rings

机译:3-甲基组胺和苯乙胺对组胺对豚鼠气管环的作用

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It is well known that histamine produces constriction via H1 receptors and decreases tracheal smooth muscle tone via H2 and H3 receptors. In addition, it has already been reported that 3-methylhistamine and phenylethylamine are competitive antagonists of histamine N-methyl-transferase (HMT), the enzyme responsible for rapid inactivation of histamine. Our results suggest the possibility that 3- methyl-histamine and phenylethylamine as competitive antagonists of histamine N-methyl-transferase lead to potentiation of histamine induced constriction of isiolated guinea-pig trachea, probably due to the decrease of histamine methylation and consequent inactivation. In as much, 3-methyl-histamine and phenylethylamine had no effect on the basal tone of isolated trachea smooth muscle, as well as on other mechanisms leading to increased responsiveness of guinea-pig tracheal smooth muscle (acetylcholine, KCl, electro stimulation).
机译:众所周知,组胺通过H1受体产生收缩,并通过H2和H3受体降低气管平滑肌张力。另外,已经报道了3-甲基组胺和苯乙胺是组胺N-甲基转移酶(HMT)的竞争性拮抗剂,该酶负责组胺的快速失活。我们的结果表明3-甲基组胺和苯乙胺作为组胺N-甲基转移酶的竞争性拮抗剂可能会增强组胺引起的碘化豚鼠气管收缩,这可能是由于组胺甲基化的减少和随之而来的失活。在大多数情况下,3-甲基组胺和苯乙胺对孤立的气管平滑肌的基调以及导致豚鼠气管平滑肌反应性增强的其他机制(乙酰胆碱,氯化钾,电刺激)没有影响。

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