Aguilar M J, Morales-Olivas F J, Rubio E
Br J Pharmacol. 1986 Jul;88(3):501-6. doi: 10.1111/j.1476-5381.1986.tb10229.x.
The effects of histamine and specific histamine agonists has been examined on isolated longitudinal colon strips of guinea-pig and rat. Histamine and 2-pyridyl-ethylamine but not 4 methylhistamine produced a concentration-related contractile response in the guinea-pig colon. The H1-antagonist clemizole antagonized competitively the effect of histamine but the H2-antagonist ranitidine did not modify the dose-response curve to histamine in the guinea-pig colon. Atropine, hexamethonium, prazosin and propranolol failed to modify the contractile response to histamine. Tone induced with KCl in guinea-pig isolated colon was not modified by histamine agonists even in tissues pretreated with clemizole or ranitidine. Histamine and histamine analogues were without effect on the isolated longitudinal strip of the rat colon. It is concluded that histamine produced dose-dependent contractions of the guinea-pig colon due to direct activation of H1-histamine receptors. There is no evidence in favour of the existence of H2-histamine receptors in this preparation. The lack of effect of histamine agonists in rat colon strip argues against the existence of histamine receptors in this preparation.
已对组胺和特定组胺激动剂对豚鼠和大鼠离体结肠纵行肌条的作用进行了研究。组胺和2-吡啶乙胺可使豚鼠结肠产生浓度依赖性收缩反应,但4-甲基组胺无此作用。H1拮抗剂氯苯咪唑可竞争性拮抗组胺的作用,但H2拮抗剂雷尼替丁并未改变豚鼠结肠对组胺的剂量反应曲线。阿托品、六甲铵、哌唑嗪和普萘洛尔均未能改变对组胺的收缩反应。即使在用氯苯咪唑或雷尼替丁预处理的组织中,组胺激动剂也不会改变豚鼠离体结肠中由氯化钾诱导的张力。组胺和组胺类似物对大鼠结肠离体纵行肌条无作用。结论是,组胺通过直接激活H1组胺受体使豚鼠结肠产生剂量依赖性收缩。没有证据支持该制剂中存在H2组胺受体。组胺激动剂对大鼠结肠肌条无作用,这与该制剂中存在组胺受体的观点相悖。