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Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells

Nature volume 274, pages 176–177 (1978)Cite this article

Abstract

TRICYCLIC antidepressants are structurally related to anti-histamines and are known to possess antihistaminic properties1. Green and co-workers2,24 showed that these drugs competitively antagonised histamine H2 receptor-mediated cyclic AMP formation by homogenates of guinea pig brain. Using muscarinic acetylcholine receptor-mediated cyclic GMP formation by mouse neuroblastoma cells (clone N1E-115)3, the interactions of psychotherapeutic drugs with this cholinergic receptor were studied in this laboratory4,5. While investigating the desensitisation of this muscarinic receptor6, it was found that histamine also stimulated cyclic GMP formation by activation of histamine H1 receptors of these cells7. This assay for histamine H1 receptors was used to obtain quantitative data for tricyclic antidepressant interactions with these receptors. This report shows that these drugs are potent competitive inhibitors of histamine H1 receptors and that some of these compounds are amongst the most potent H1 antagonists known.

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  1. Departments of Psychiatry and Pharmacology, Mayo Foundation, Rochester, Minnesota, 55901

    ELLIOTT RICHELSON

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RICHELSON, E. Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells. Nature 274, 176–177 (1978). https://doi.org/10.1038/274176a0

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