Tricyclic antidepressants: Potent blockade of histamine H1 receptors of guinea pig ileum

James Figge, Paul Leonard, Elliott Richelson

Research output: Contribution to journalArticlepeer-review

25 Scopus citations


Six tricyclic antidepressants were tested for their ability to antagonize histamine actions at histamine H1 receptors in a bioassay for these receptors (histamine-induced contractions of guinea pig ileum). All compounds were competitive antagonists with equilibrium dissociation constants in the range of 5.6 x 10-11 M to 1.5 x 10-7 M. Doxepin hydrochloride and amitriptyline hydrochloride were the most potent compounds of the series and may be the most potent antihistamines known. Antagonism at histamine H1 receptors by these compounds may explain their sedative effects.

Original languageEnglish (US)
Pages (from-to)479-483
Number of pages5
JournalEuropean Journal of Pharmacology
Issue number4
StatePublished - Oct 15 1979

ASJC Scopus subject areas

  • Pharmacology


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