[3H]mianserin

Differential labeling of serotonin2 and histamine1 receptors in rat brain

S. J. Peroutka, Solomon H Snyder

Research output: Contribution to journalArticle

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

Fingerprint

Mianserin
Histamine H1 Receptors
Brain
Membranes
Triprolidine
Histamine H1 Antagonists
Spiperone
Cerebrum
Cerebellum
Antidepressive Agents
Smooth Muscle
Serotonin
Guinea Pigs
Binding Sites

ASJC Scopus subject areas

  • Pharmacology

Cite this

[3H]mianserin : Differential labeling of serotonin2 and histamine1 receptors in rat brain. / Peroutka, S. J.; Snyder, Solomon H.

In: Journal of Pharmacology and Experimental Therapeutics, Vol. 216, No. 1, 1981, p. 142-148.

Research output: Contribution to journalArticle

@article{afbcd2ee353a4d21aca3268db9840286,
title = "[3H]mianserin: Differential labeling of serotonin2 and histamine1 receptors in rat brain",
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.",
author = "Peroutka, {S. J.} and Snyder, {Solomon H}",
year = "1981",
language = "English (US)",
volume = "216",
pages = "142--148",
journal = "Journal of Pharmacology and Experimental Therapeutics",
issn = "0022-3565",
publisher = "American Society for Pharmacology and Experimental Therapeutics",
number = "1",

}

TY - JOUR

T1 - [3H]mianserin

T2 - Differential labeling of serotonin2 and histamine1 receptors in rat brain

AU - Peroutka, S. J.

AU - Snyder, Solomon H

PY - 1981

Y1 - 1981

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0019391578&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0019391578&partnerID=8YFLogxK

M3 - Article

VL - 216

SP - 142

EP - 148

JO - Journal of Pharmacology and Experimental Therapeutics

JF - Journal of Pharmacology and Experimental Therapeutics

SN - 0022-3565

IS - 1

ER -