Abstract
The first radioligand used in an attempt to label receptors for 5-hydroxytryptamine (5-HT) receptors in the CNS was [3H]-5-HT (March-banks, 1966). It was not until 1976, however, that a specific population of high-affinity, saturable binding sites in brain membranes was identified using this radioligand by Bennett and Snyder (1976). In 1979, it was determined that the binding sites labelled by [3H]-5-HT were distinct from a second class of 5-HT binding sites labelled by [3H]-spiperone (Peroutka and Snyder, 1979; Peroutka et al., 1981). The sites labelled by [3H]-5-HT were designated 5-HT1 binding sites, and initially were believed to be homogeneous.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Bennett, J. P., Jr and Snyder, S. H. (1976). Serotonin and lysergic acid diethylamide binding in rat brain membranes: Relationship to postsynaptic serotonin receptors. Mol Pharmacol, 12, 373–389
Blurton, P. A. and Wood, M. D. (1986). Identification of multiple binding sites for [3H]5-hydroxytryptamine in the rat CNS. J. Neurochem., 46, 1392–1398
Charlton, K. G., Bond, R. A. and Clarke, D. E. (1986). An inhibitory prejunctional 5-HT1-like receptor in the isolated perfused rat kidney. Naunyn-Schmiedeberg’s Arch. Pharmacol, 332, 8–15
Clineschmidt, B. V., Reiss, D. R., Pettibone, J. and Robinson, J. L. (1985). Characterization of 5-hydroxytryptamine receptors in rat stomach fundus. J. Pharmacol. Exp. Ther., 235, 696–708
Cohen, M. L. and Wittenauer, L. A. (1986). Further evidence that the serotonin receptor in the rat stomach fundus is not 5-HT1A or 5-HT1B. Life Sci., 38, 1–5
Conn, P. J., Sanders-Bush, E., Hoffman, B. J. and Hartig, P. R. (1986). A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover. Proc. Natl Acad. Sci. U.S.A, 83, 4086–4088
De Vivo, M. and Maayani, S. (1986). Characterization of the 5-hydroxytryptamine1A receptor-mediated inhibition of forskolin-stimulated adeny-late cyclase activity in guinea pig and rat hippocampal membranes. J. Pharmacol. Exp. Ther., 238, 248–253
Doods, H. N., Kalkman, H. O., De Jonge, A., Thoolen, M., Wilffert, B., Timmermans, P. and Van Zwieten, P. A. (1985). Differential selectivities of RU 24969 and 8-OH-DPAT for the purported 5-HT1A and 5-HT1B binding sites. Correlation between 5-HT1A affinity and hypotensive activity. Eur. J. Pharmacol., 112, 363–370
Engel, G., Göthert, M., Hoyer, D., Schlicker, E. and Hillenbrand, K. (1986). Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites. Naunyn-Schmiedeberg’s Arch. Pharmacol, 357, 1–7
Gudelsky, G. A., Koenig, J. I. and Meltzer, H. Y. (1986). Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Neuropharmacolo-gy, 25, 1307–1313
Heuring, R. E. and Peroutka, S. J. (1987). Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes. J. Neurosci., 7, 894–903
Heuring, R. E., Schlegel, J. R. and Peroutka, S. J. (1986). Species variations in 5-HT1B and 5-HT1C binding sites defined by RU 24969 competition studies. Eur. J. Pharmacol, 122, 279–282
Hoyer, D., Engel, G. and Kalkman, H. O. (1985). Characterization of the 5-HT1Brecognition site in rat brain: Binding studies with (−)[125I] iodocyanopindolol. Eur. J. Pharmacol., 118, 1–12
Hoyer, D., Pazos, A., Probst, A. and Palacios, J. M. (1986). Serotonin receptors in the human brain: I. Characterization and autoradiographic localization of 5-HT1Arecognition sites. Apparent absence of 5-HT1B recognition sites. Brain Res., 376, 85–96
Kwong, L. L., Smith, E. R., Davidson, J. M. and Peroutka, S. J. (1986). Differential interactions of ‘prosexual’ drugs with 5-hydroxytryptamine1A and alpha2-adrenergic receptors. Behav. Neurosci., 100, 664–668
Marchbanks, R. M. (1966). Serotonin binding to nerve ending particles and other preparations from rat brain. J. Neurochem., 13, 1481–1493
Marcinkiewicz, M., Vergé, D., Gozlan, H., Pichat, L. and Hamon, M. (1984). Autoradiographic evidence for the heterogeneity of 5-HT1 sites in the rat brain. Brain Res., 291, 159–163
Markstein, R., Hoyer, D. and Engel, G. (1986). 5-HT1A receptors mediate stimulation of adenylate cyclase in rat hippocampus. Naunyn-Schmiedeberg’s Arch. Pharmacol, 333, 335–341
Pazos, A. and Palacios, J. M. (1985). Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptors. Brain Res., 346, 205–230
Pazos, A., Hoyer, D. and Palacios, J. M. (1985). The binding of serotonergic ligands to the porcine choroid plexus: Characterization of a new type of serotonin recognition site. Eur. J. Pharmacol., 106, 539–546
Pedigo, N. W., Yamamura, H. I. and Nelson, D. L. (1981). Discrimination of multiple [3H]5-hydroxytryptamine binding sites by the neuroleptic spiperone in rat brain. J. Neurochem., 36, 220–226
Peroutka, S. J. (1986). Pharmacological differentiation and characterization of 5-HT1A, 5-HT1B and 5-HT1C binding sites in rat frontal cortex. J. Neurochem., 47, 529–540
Peroutka, S. J. (1988). 5-Hydroxytryptamine receptor subtypes. Ann. Rev. Neurosci., 11, 45–60
Peroutka, S. J. and Snyder, S. H. (1979). Multiple serotonin receptors: differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol. Mol. Pharmacol., 16, 687–699
Peroutka, S. J., Lebovitz, R. M. and Snyder, S. H. (1981). Two distinct central serotonin receptors with different physiological functions. Science, 212, 827–829
Peroutka, S. J., Huang, S. and Allen, G. S. (1986). Canine basilar artery contractions mediated by 5-hydroxytryptamine1A receptors. J. Pharmacol. Exp. Ther., 237, 901–906
Raiteri, M., Maura, G., Bonanno, G. and Pittaluga, A. (1986). Differential pharmacology and function of two 5-HT1 receptors modulating transmitter release in cerebellum. J. Pharmacol. Exp. Ther., 237, 644–648
Schnellmann, R. G., Waters, S. J. and Nelson, D. L. (1984). [3H]5-Hydroxy-tryptamine binding sites: Species and tissue variation. J. Neurochem., 42, 65–70
Smith, L. M. and Peroutka, S. J. (1986). Differential effects of 5-hydroxy-tryptamine1A selective drugs on the 5-HT-behavioral syndrome. Pharmacol. Biochem. Behav., 24, 1513–1519
Sprouse, J. S. and Aghajanian, G. K. (1987). Electrophysiological responses of serotonergic dorsal raphe neurons to 5-HT1A and 5-HT1B agonists. Synapse, 1, 3–9
Taylor, E. W., Duckies, S. P. and Nelson, D. L. (1986). Dissociation constants of serotonin agonists in the canine basilar artery correlate to Ki values at the 5-HT1Abinding site. J. Pharmacol. Exp. Ther., 236, 118–125
Tricklebank, M. D., Forler, C. and Fozard, J. R. (1984). The involvement of subtypes of the 5-HT1 receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino)tetralin in the rat. Eur. J. Pharmacol., 106, 271–282
Tricklebank, M. D., Forler, C., Middlemiss, D. N. and Fozard, J. R. (1985). Subtypes of the 5-HT receptor mediating the behavioural responses to 5-methoxy-N,N-dimethyltryptamine in the rat. Eur. J. Pharmacol., 117, 15–24
Tricklebank, M. D., Middlemiss, D. N. and Neill, J. (1986). Pharmacological analysis of the behavioral and thermoregulatory effects of the putative 5-HT1receptor agonist, RU 24969, in the rat. Neuropharmacology, 25, 877–886
Trulson, M. E. and Arasteh, K. (1986). Buspirone decreases the activity of 5-hydroxytryptamine-containing dorsal raphe neurons in-vitro. J. Pharm. Pharmacol., 38, 380–382
VanderMaelen, C. P., Matheson, G. K., Wilderman, R. C. and Patterson, L. A. (1986). Inhibition of serotonergic dorsal raphe neurons by systemic and iontophoretic administration of buspirone, a non-benzodiazepine anxiolytic drug. Eur. J. Pharmacol., 129, 123–130
Yagaloff, K. A. and Hartig, P. R. (1985). 125I-LSD binds to a novel serotonergic site on rat choroid plexus epithelial cells. J. Neurosci., 5, 3178–3183
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Copyright information
© 1989 The editors and contributors
About this chapter
Cite this chapter
Peroutka, S.J. (1989). Characterization of 5-HT1 Binding Site Subtypes Labelled by [3H]-5-Hydroxytryptamine. In: Mylecharane, E.J., Angus, J.A., de la Lande, I.S., Humphrey, P.P.A. (eds) Serotonin. Satellite Symposia of the IUPHAR 10th International Congress of Pharmacology. Palgrave Macmillan, London. https://doi.org/10.1007/978-1-349-10114-6_24
Download citation
DOI: https://doi.org/10.1007/978-1-349-10114-6_24
Publisher Name: Palgrave Macmillan, London
Print ISBN: 978-1-349-10116-0
Online ISBN: 978-1-349-10114-6
eBook Packages: Biomedical and Life SciencesBiomedical and Life Sciences (R0)