Effects of antidepressant drugs on histamine-H1 receptors in the brain.
The histamine-H1 receptor blocking properties of a number of structurally different antidepressant drugs have been evaluated using a 3H-mepyramine binding assay and a guinea-pig ileum preparation. The tricyclic antidepressants all inhibited the histamine-H1 receptor. Some newer antidepressant drugs, such as zimelidine and nomifensine were devoid of activity while others, such as iprindole and mianserin were very potent. It is concluded that antagonistic effects on the histamine-H1 receptor is not associated with the therapeutic efficacy in depression, but may contribute to the sedative effects of the antidepressant drugs.
D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology; D001921:Brain / Q000187:drug effects*; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D007082:Ileum / Q000378:metabolism; D008297:Male; D010632:Pheniramine / Q000378:metabolism; D011738:Pyrilamine / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011968:Receptors, Histamine / Q000187:drug effects*; D011969:Receptors, Histamine H1 / Q000187:drug effects*; D015031:Zimeldine / Q000378:metabolism
D000928:Antidepressive Agents; D000929:Antidepressive Agents, Tricyclic; D006634:Histamine H1 Antagonists; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D010632:Pheniramine; D015031:Zimeldine; D011738:Pyrilamine