Alvarez F J, Casas E, Carvajal A, Velasco A
J Pharmacol. 1986 Apr-Jun;17(2):149-54.
The properties of some tricyclic and non-tricyclic antidepressants on antagonist histamine H1 and muscarinic acetylcholine receptors have been evaluated on guinea-pig ileum. They act like competitive antagonists on histamine H1 receptors. Some of them show a competitive antagonism and others a non-competitive antagonism on muscarinic acetylcholine receptors. A few of them are very potent antagonists on histamine H1 and/or muscarinic acetylcholine receptors, while others, especially the non-tricyclic antidepressants, have a small potency. All antidepressants have a higher histamine H1 activity than muscarinic acetylcholine activity. These results cannot explain the therapeutic effect of these drugs, but they can account for some side effects and drug interactions.
已在豚鼠回肠上评估了一些三环类和非三环类抗抑郁药对组胺H1和毒蕈碱型乙酰胆碱受体拮抗剂的特性。它们在组胺H1受体上表现为竞争性拮抗剂。其中一些对毒蕈碱型乙酰胆碱受体表现出竞争性拮抗作用，而另一些则表现出非竞争性拮抗作用。它们中的一些对组胺H1和/或毒蕈碱型乙酰胆碱受体是非常有效的拮抗剂，而另一些，尤其是非三环类抗抑郁药，效力较小。所有抗抑郁药的组胺H1活性均高于毒蕈碱型乙酰胆碱活性。这些结果无法解释这些药物的治疗效果，但可以解释一些副作用和药物相互作用。
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