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Multiple Serotonin Receptors: Differential Binding of [3H]5-Hydroxytryptamine, [3H]Lysergic Acid Diethylamide and [3H]Spiroperidol
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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Cited by
Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine
Bradley, P. B., Engel, G., Feniuk, W., Fozard, J. R., Humphrey, P. P. A., Middlemiss, D. N., Mylecharane, E. J., Richardson, B. P., & Saxena, P. R. (1986) · Neuropharmacology · doi:10.1016/0028-3908(86)90207-8 · Cited by 1,258
Molecular biology of 5-HT receptors
Hannon, J., & Hoyer, D. (2008) · Behavioural Brain Research · doi:10.1016/j.bbr.2008.03.020 · Cited by 815
Serotonin and brain function: a tale of two receptors
Carhart-Harris, R., & Nutt, D. (2017) · Journal of Psychopharmacology · doi:10.1177/0269881117725915 · Cited by 739
López, J. F., Chalmers, D. T., Little, K. Y., & Watson, S. J. (1998) · Biological Psychiatry · doi:10.1016/s0006-3223(97)00484-8 · Cited by 699
Charney, D. S. (1981) · Archives of General Psychiatry · doi:10.1001/archpsyc.1981.01780350094011 · Cited by 649
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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