Abstract
The history of the development of our overall understanding of the classification of receptors for 5-hydroxytryptamine (5-HT) was extensively discussed by the participants at the workshop on 5-HT receptor classification. The general consensus was that, despite major recent advances, a clear picture has yet to emerge because specific drug tools are not available to characterize definitively all the known/putative 5-HT receptor types. Furthermore, although all the workshop participants expressed a general desire to collate data from functional studies with data from ligand binding studies, this is not always as easy as it has been with the 5-HT2 receptor. Nevertheless, despite these shortcomings, it was agreed that the attempted all-embracing 5-HT receptor classification of Bradley et al. (1986) still provided a framework of understanding on which to build. Indeed, the majority of new data presented reinforced the classification, although some observations were difficult to encompass within it.
This overview incorporates material presented during the classification of 5-HT receptors and binding sites session, and material discussed in a workshop chaired by the authors; an attempt has been made to reflect all the views expressed and not just those of the authors (see acknowledgements).
This is a preview of subscription content, log in via an institution to check access.
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
Bradley, P. B., Engel, G., Feniuk, W., Fozard, J. R., Humphrey, P. P. A., Middlemiss, D. N., Mylecharane, E. J., Richardson, B. P. and Saxena, P. R. (1986). Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology, 25, 563–576
Buchheit, K. H., Engel, G., Mutschier, E. and Richardson, B. P. (1985). Study of the contractile effect of 5-hydroxytryptamine (5-HT) in the isolated longitudinal muscle strip from guinea-pig ileum. Evidence for two distinct release mechanisms. Naunyn-Schmiedeberg’s Arch. Pharmacol., 329, 36–41
Charlton, K. G., Bond, R. A. and Clarke, D. E. (1986). An inhibitory prejunctional 5-HT1-like receptor in the isolated perfused rat kidney. Apparent distinction from the 5-HT1A, 5-HT1B and 5-HT1C subtypes. Naunyn-Schmiedeberg’s Arch. Pharmacol., 332, 8–15
Cocks, T. M. and Angus, J. A (1983). Endothelium-dependent relaxation of coronary arteries by noradrenaline and serotonin. Nature, 305, 627–630
Conn, P. J., Sanders-Bush, E., Hoffmann, 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
Connor, H. E., Feniuk, W., Humphrey, P. P. A. and Perren, M. J. (1986). 5-Carboxamidotryptamine is a selective agonist at 5-hydroxytryptamine receptors mediating vasodilatation and tachycardia in anaesthetized cats. Br. J. Pharmacol., 87, 417–426
Costall, B., Domeney, A. M., Naylor, R. J. and Tyers, M. B. (1987). Effects of the 5-HT3 receptor antagonist, GR 38032F, on raised dopaminergic activity in the mesolimbic system of the rat and marmoset brain. Br. J. Pharmacol., 92, 881–894
Dalton, D. W., Feniuk, W. and Humphrey, P. P. A. (1986). An investigation into the mechanisms of the cardiovascular effects of 5-hydroxytryptamine in conscious normotensive and doca-salt hypertensive rats. J. Auton. Pharmacol., 6, 219–228
Engel, G., Göthert, M., Müller-Schweinitzer, E., Schlicker, E., Sistonen, L. and Stadler, P. A. (1983). Evidence for common pharmacological properties of [3H]5-hydroxytryptamine binding sites, presynaptic 5-hydroxytryptamine autore-ceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors on sympathetic nerves. Naunyn-Schmiedeberg’s Arch. Pharmacol., 324, 116–124
Engel, G., Hoyer, D., Kalkman, H. O. and Wick, M. B. (1984). Identification of 5-HT2 receptors on longitudinal muscle of the guinea pig ileum. J. Recep. Res., 4, 113–126
Feniuk, W., Humphrey, P. P. A. and Watts, A. D. (1983). 5-Hydroxytryptamine-induced relaxation of isolated mammalian smooth muscle. Eur. J. Pharmacol., 96, 71–78
Fozard, J. R. (1984). MDL 72222, a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors. Naunyn-Schmiedeberg’s Arch. Pharmacol., 326, 35–44
Gunning, S. J. and Humphrey, P. P. A. (1987). Evidence for 5-HT3-receptor mediated release of an inhibitory transmitter in guinea-pig isolated ileum. Br. J. Pharmacol., 91, 359P
Heuring, R. E. and Peroutka, S. J.(1987). Characterization of a novel 3H-5-hydroxytryptamine binding site in bovine brain membranes. J. Neurosci., 7, 894–903
Holt, S. E., Cooper, M. and Wyllie, J. H. (1986). On the nature of the receptor mediating the action of 5-hydroxytryptamine in potentiating responses of the mouse urinary bladder strip to electrical stimulation. Naunyn-Schmiedeberg’s Arch. Pharmacol., 334, 333–340
Hoyer, D. and Schoeffter, P. (1988). 5-HT1D receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in calf substantia nigra. Eur. J. Pharmacol., 147, 145–147
Hoyer, D., Pazos, A., Probst, A. and Palacios, J. M. (1986a). 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
Hoyer, D., Pazos, A., Probst, A. and Palacios, J. M. (1986b). Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition site’s. Brain Res., 376, 97–107
Humphrey, P. P. A. and Feniuk, W. (1987a). Classification of functional 5-hydroxytryptamine receptors. In Rand, M. J. and Raper, C. (Eds), Pharmacology, Proceedings of the Xth International Congress of Pharmacology, Sydney, Elsevier, Amsterdam, pp. 277–280
Humphrey, P. P. A. and Feniuk, W. (1987b). Pharmacological characterisation of functional neuronal receptors for 5-hydroxytryptamine. In Nobin, A., Owman, Ch. and Arneklo-Nobin, B. (Eds), Neuronal Messengers in Vascular Function, Fernström Foundation Series, Vol. 10, Elsevier, Amsterdam, pp. 3–19
Humphrey, P. P. A., Feniuk, W., Perren, M. J., Oxford, A. W., Brittain, R. T. and Jack, D. (1987a). The pharmacology of selective 5-HT1-like receptor agonists for the acute treatment of migraine. Cephalalgia, 7, 400–401
Humphrey, P. P. A., Feniuk, W., Perren, M. J., Oxford, A. W., Coates, I. H., Butina, D., Brittain, R. T. and Jack, D. (1987b). GR 43175 — A selective agonist for functional 5-HT1-like receptors in dog saphenous vein. Br. J. Pharmacol., 92, 616P
Humphrey, P. P. A., Feniuk, W., Perren, M. J., Connor, H., Oxford, A. W., Coates, I. H. and Butina, D. (1988). GR 43175, a selective agonist for the 5-HT1-like receptor in dog isolated saphenous vein. Br. J. Pharmacol., 94, 1123–1132
Kilpatrick, G. J., Jones, B. J. and Tyers, M. B. (1987). Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding. Nature, 330, 746–748
Leff, P. and Martin, G. R. (1986). Peripheral 5-HT2-like receptors. Can they be classified with the available antagonists? Br. J. Pharmacol., 88, 585–593
Leff, P., Martin, G.R. and Morse, J. M. (1987). Differential classification of vascular smooth muscle and endothelial cell 5-HT receptors by use of tryptamine analogues. Br. J. Pharmacol., 91, 321–331
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
Martin, K. F. and Mason, R. (1987). Ipsapirone is a partial agonist at 5-hydroxytryptamine 1A (5-HT1A) receptors in the rat hippocampus: electrophy-siological evidence. Eur. J. Pharmacol., 141, 479–483
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
Richardson, B. P. and Engel, G. (1986). The pharmacology and function of 5-HT3receptors. Trends in Neurosci., 9, 424–428
Richardson, B. P., Engel, G., Donatsch, P. and Stadler, P. A. (1985). Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs. Nature, 316, 126–131
Shenker, A., Maayani, S., Weinstein, H. and Green, J. P. (1985). Two 5-HT receptors linked to adenylate cyclase in guinea-pig hippocampus are discriminated by 5-carboxyamidotryptamine and spiperone. Eur. J. Pharmacol., 109, 427–429
Stephenson, R. P. (1975). Interaction of agonists and antagonists with their receptors. INSERM, 50, 15–28
Sumner, M. J., Humphrey, P. P. A. and Feniuk, W. (1987). Characterisation of the 5-HT1-like receptor mediating relaxation of porcine vena cava. Br. J. Pharmacol., 92, 574P
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Copyright information
© 1989 The editors and contributors
About this chapter
Cite this chapter
Humphrey, P.P.A., Richardson, B.P. (1989). Classification of 5-HT Receptors and Binding Sites: An Overview. 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_26
Download citation
DOI: https://doi.org/10.1007/978-1-349-10114-6_26
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)