Heterogeneity of histamine H1-receptors

species variations in [3H]mepyramine binding of brain membranes

R. S L Chang, V. T. Tran, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

[3H]Mepyramine binds with high affinity to membranes from brain of human, rat, guinea pig, rabbit and mouse with drug specificity indicating an association with histamine H1, receptors. Considerable species differences occur in the affinity of [3H]mepyramine, with guinea-pig and human having 3-6 times greater affinity than rat, mouse or rabbit. The greater affinity of [3H]mepyramine in guinea-pig than in rat is attributable both to faster association and slower dissociation rates in guinea-pig. Species differences in affinity for H1 receptor sites occur for some antihistamines but not for others. Some tricyclic antidepressant and neuroleptic drugs are extremely potent inhibitors of [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined. The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding. The regional distribution of specific [3H]mepyramine binding differs considerably in the various species examined.

Original languageEnglish (US)
Pages (from-to)1653-1663
Number of pages11
JournalJournal of Neurochemistry
Volume32
Issue number6
StatePublished - 1979

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Pyrilamine
Histamine H1 Receptors
Brain
Membranes
Guinea Pigs
Rats
Tricyclic Antidepressive Agents
Histamine Antagonists
Antipsychotic Agents
Doxepin
Association reactions
Rabbits
Clozapine
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience

Cite this

Heterogeneity of histamine H1-receptors : species variations in [3H]mepyramine binding of brain membranes. / Chang, R. S L; Tran, V. T.; Snyder, Solomon H.

In: Journal of Neurochemistry, Vol. 32, No. 6, 1979, p. 1653-1663.

Research output: Contribution to journalArticle

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