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Multiple Serotonin Receptors: Differential Binding of [3H]5-Hydroxytryptamine, [3H]Lysergic Acid Diethylamide and [3H]Spiroperidol

PEROUTKA, STEPHEN J., SNYDER, SOLOMON H.·1979·Molecular Pharmacology

Abstract

[3H]5-Hydroxytryptamine (5-HT), [3H]lysergic acid diethylamide (LSD) and [3H]spiroperidol bind to membranes from the rat frontal cerebral cortex in a manner indicating a selective interaction with serotonin receptors. Differential drug potencies in competing for [3H]5-HT and [3H]spiroperidol binding sites suggest that these two [3H]ligands respectively label two distinct populations of receptors, while [3H]LSD labels both the [3H]5-HT and [3H]spiroperidol sites. After incubation of brain membranes with 30 nM spiroperidol, drug specificity of the residual [3H]LSD binding resembles that of receptors labeled by [3H]5-HT. Conversely, drug effects on [3H]LSD binding in the presence of 300 nM 5-HT resemble effects with [3H]spiroperidol. We propose that [3H]5-HT and [3H]-spiroperidol label distinct populations of serotonin receptors in rat brain, designated 5-HT1 and 5-HT2 receptors, respectively. [3H]LSD appears to bind to both receptors to a similar extent. ACKNOWLEDGMENTS We thank Richard M. Lebovitz for his skillful technical assistance and Pamela Morgan for manuscript preparation.

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Metadata

Authors
PEROUTKA, S. J., & SNYDER, S. H.
Venue
Molecular Pharmacology
Publisher
Elsevier BV
Published
1979-11
Volume
16
Issue
3
Pages
687-699
ISSN
0026-895X (ISSN-L)
OpenAlex
W2341140535
Cited by
1,360
References
0
FWCI
14.23
Type
journal article
Language
en
Open access
closed

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CoChat. (2026). Citation check: Multiple Serotonin Receptors: Differential Binding of [3H]5-Hydroxytryptamine, [3H]Lysergic Acid Diethylamide and [3H]Spiroperidol. https://app.cochat.ai/papers/10.1016/s0026-895x(25)13812-1
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PEROUTKA, S. J., & SNYDER, S. H. (1979). Multiple Serotonin Receptors: Differential Binding of [3H]5-Hydroxytryptamine, [3H]Lysergic Acid Diethylamide and [3H]Spiroperidol. Molecular Pharmacology. https://doi.org/10.1016/s0026-895x(25)13812-1

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