[3H]mianserin: Differential labeling of serotonin2 and histamine1 receptors in rat brain

S. J. Peroutka, S. H. Snyder

Research output: Contribution to journalArticlepeer-review

Abstract

Mianserin, a tetracyclic antidepressant, is a potent serotinin (5-HT) and histamine H1 antagonist in peripheral smooth muscle systems. Mianserin was found to possess high affinity for 5-HT2 and histamine H1 receptor binding sites in brain membranes. By using [3H]mianserin, both 5-HT2 and histamine H1 receptors can be specifically labeled in rat cerebra cortex membranes. Simultaneous incubation of brain membranes with 300 nM triprolidine or 30 nM spiroperidol enables the selective labeling of 5-HT2 or histamine H1 receptors, respectively. In the guinea-pig cerebellum, [3H]mianserin exclusively labels histamine H1 receptors, since 5-HT2 sites are virtually absent in this area.

Original languageEnglish (US)
Pages (from-to)142-148
Number of pages7
JournalJournal of Pharmacology and Experimental Therapeutics
Volume216
Issue number1
StatePublished - 1981

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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