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

James Figge, Paul Leonard, Elliott Richelson

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

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
Volume58
Issue number4
DOIs
StatePublished - Oct 15 1979

Fingerprint

Histamine H1 Receptors
Tricyclic Antidepressive Agents
Ileum
Guinea Pigs
Doxepin
Histamine Receptors
Amitriptyline
Histamine Antagonists
Hypnotics and Sedatives
Biological Assay
Histamine

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Tricyclic antidepressants : Potent blockade of histamine H1 receptors of guinea pig ileum. / Figge, James; Leonard, Paul; Richelson, Elliott.

In: European Journal of Pharmacology, Vol. 58, No. 4, 15.10.1979, p. 479-483.

Research output: Contribution to journalArticle

Figge, James ; Leonard, Paul ; Richelson, Elliott. / Tricyclic antidepressants : Potent blockade of histamine H1 receptors of guinea pig ileum. In: European Journal of Pharmacology. 1979 ; Vol. 58, No. 4. pp. 479-483.
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