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5-HT Receptors Mediating Pre-synaptic Autoinhibition in Central Serotoninergic Nerve Terminals

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Serotonin

Abstract

Pre-synaptic 5-HT autoreceptors are receptors which are located on (or at least close to) the axon terminals of serotoninergic neurones. Accordingly, they can be activated by serotonin (5-hydroxytryptamine; 5-HT) released from those terminals on which they are located. It is compatible with this location that 5-HT autoreceptors probably play a physiological role in fine regulation of 5-HT release (and of 5-HT synthesis: Hamon et al., 1973; Sawada and Nagatsu, 1986).

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References

  • Baumann, P. A. and Waldmeier, P. C. (1981). Further evidence for negative feedback control of serotonin release in the central nervous system. Naunyn-Schmiedeberg’s Arch. Pharmacol., 317, 36–43

    Google Scholar 

  • Bonanno, G., Maura, G. and Raiteri, M. (1986). Pharmacological characterization of release-regulating serotonin autoreceptors in rat cerebellum. Eur. J. Pharmacol., 126, 317–321

    Google Scholar 

  • Brazell, M. P., Marsden, C. C., Nisbet, A. P. and Routledge, C. (1985). The 5-HT1receptor agonist RU-24969 decreases 5-hydroxytryptamine (5-HT) release and metabolism in the rat frontal cortex in vitro and in vivo. Br. J. Pharmacol., 86, 209–216

    Google Scholar 

  • Cerrito, F. and Raiteri, M. (1979). Serotonin release is modulated by presynaptic autoreceptors. Eur. J. Pharmacol., 57, 427–430

    Google Scholar 

  • Chaput, Y., Blier, P. and De Montigny, C. (1986). In vivo electrophysiological evidence for the regulatory role of autoreceptors on serotonergic terminals. J. Neurosci., 6, 2796–2801

    Google Scholar 

  • 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 autoreceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors on sympathetic nerves. Naunyn-Schmiedeberg’s Arch. Pharmacol., 324, 116–124

    Google Scholar 

  • Engd, 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., 332, 1–7

    Google Scholar 

  • Feuerstein, T. J., Lupp, A. and Hertting, G. (1987). The serotonin (5-HT) autoreceptor in the hippocampus of the rabbit: role of 5-HT biophase concentration. Neuropharmacology, 26, 1077–1080.

    Google Scholar 

  • Figueroa, H. R., Yürgens, P. B., Newton, D. K and Hall, T. R. (1985). Evidence for negative feedback control of the release of [3H] serotonin from superfused mouse cerebellum slices induced by electrical field stimulation. Gen. Pharmacol., 16, 103–108

    Google Scholar 

  • Göthert, M. (1980). Serotonin-receptor-mediated modulation of Ca2+-dependent 5-hydroxytryptamine release from neurones of the rat brain cortex. Naunyn-Schmiedeberg’s Arch. Pharmacol., 314, 223–230

    Google Scholar 

  • Göthert, M. (1982). Modulation of serotonin release in the brain via presynaptic receptors. Trends in Pharmacol. Sci., 3, 437–440

    Google Scholar 

  • Göthert, M. (1985). Role of autoreceptors in the function of the peripheral and central nervous system. Arzneimittelforschung, 35, 1909–1916

    Google Scholar 

  • Göthert, M. (1986). Presynaptic 5-HT autoreceptors and the modulation of the release of 5-HT. Clin. Neuropharmacol., 9, Suppl. 4, 308–310

    Google Scholar 

  • Göthert, M. and Schlicker, E. (1983). Autoreceptor-mediated inhibition of 3H-5-hydroxytryptamine release from rat brain cortex slices by analogues of 5-hydroxytryptamine. Life Sci., 32, 1183–1191

    Google Scholar 

  • Göthert, M. and Weinheimer, G. (1979). Extracellular 5-hydroxytryptamine inhibits 5-hydroxytryptamine release from rat brain cortex slices. Naunyn-Schmiedeberg’s Arch. Pharmacol., 310, 93–96

    Google Scholar 

  • Hamon, M., Bourgoin, S. and Glowinski, J. (1973). Feedback regulation of 5-HT synthesis in rat striatal slices. J. Neurochem., 20, 1727–1745

    Google Scholar 

  • Héry, F., Simonnet, G., Bourgoin, S., Soubrié, P., Artaud, F., Hamon, M. and Glowinski, J. (1979). Effect of nerve activity on the in vivo release of [3H] serotonin continuously formed from L-[3H] tryptophan in the caudate nucleus of the cat. Brain Res., 169, 317–334

    Google Scholar 

  • Langer, S. Z. and Moret, C. (1982). Citalopram antagonizes the stimulation by lysergic acid diethylamide of presynaptic inhibitory serotonin autoreceptors in the rat hypothalamus. J. Pharmacol. Exp. Ther., 222, 220–226

    Google Scholar 

  • Limberger, N., Bonanno, G., Späth, L. and Starke, K. (1986). Autoreceptors and α2-adrenoceptors at the serotonergic axons of rabbit brain cortex. Naunyn-Schmiedeberg’s Arch. Pharmacol., 332, 324–331

    Google Scholar 

  • Martin, L. L. and Sanders-Bush, E. (1982). Comparison of the pharmacological characteristics of 5-HT1 and 5-HT2 binding sites with those of serotonin autoreceptors which modulate serotonin release. Naunyn-Schmiedeberg’s Arch. Pharmacol., 321, 165–170

    Google Scholar 

  • Maura, G., Roccatagliata, E. and Raiteri, M. (1986). Serotonin autoreceptor in rat hippocampus: Pharmacological characterization as a subtype of the 5-HT1receptor. Naunyn-Schmiedeberg’s Arch. Pharmacol., 334, 323–326

    Google Scholar 

  • Maura, G., Ulivi, M. and Raiteri, M. (1987). (−)-Propranolol and (±)-cyanopindolol are mixed agonists—antagonists at serotonin autoreceptors in the hippocampus of the rat brain. Neuropharmacology, 26, 713–717

    Google Scholar 

  • Middlemiss, D. N. (1984a). 8-Hydroxy-2-(di-n-propylamino)tetralin is devoid of activity at the 5-hydroxytryptamine autoreceptor in rat brain. Implications for the proposed link between the autoreceptor and the [3H]5-HT recognition site. Naunyn-Schmiedeberger’s Arch. Pharmacol., 327, 18–22

    Google Scholar 

  • Middlemiss, D. N. (1984b). Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol. Eur. J. Pharmacol., 101, 289–293

    Google Scholar 

  • Monroe, P. J. and Smith, D. J. (1985). Demonstration of an autoreceptor modulating the release of [3H]5-hydroxytryptamine from a synaptosomal-rich spinal cord tissue preparation. J. Neurochem., 45, 1886–1894

    Google Scholar 

  • Moret, C. (1985). Pharmacology of the serotonin autoreceptor. In Green, A. R. (Ed.), Neuropharmacology of Serotonin, Oxford University Press, Oxford, pp. 21–49

    Google Scholar 

  • Neale, R. F., Fallon, S. L., Boyar, W. C., Wasley, J. W. F., Martin, L. L., Stone, G. A., Glaeser, B. S., Sinton, C. M. and Williams, M. (1987). Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. Eur. J. Pharmacol., 136, 1–9

    Google Scholar 

  • Raiteri, M., Bonnano, G., Marchi, M. and Maura, G. (1984). Is there a functional linkage between neurotransmitter uptake mechanisms and presynaptic receptors? J. Pharmacol. Exp. Ther., 231, 671–677

    Google Scholar 

  • Sawada, M. and Nagatsu, T. (1986). Stimulation of the serotonin autoreceptor prevents the calcium-calmodulin-dependent increase of serotonin biosynthesis in rat raphe slices. J. Neurochem., 46, 963–967

    Google Scholar 

  • Schlicker, E., Göthert, M. and Hillenbrand, K. (1985a). Cyanopindolol is a highly potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Naunyn-Schmiedeberg’s Arch. Pharmacol., 331, 398–401

    Google Scholar 

  • Schlicker, E., Brandt, F., Classen, K. and Göthert, M. (1985b). Serotonin release in human cerebral cortex and its modulation via serotonin receptors. Brain Res., 331, 337–341

    Google Scholar 

  • Schlicker, E., Fink, K., Classen, K. and Göthert, M. (1987). Facilitation of serotonin (5-HT) release in the rat brain cortex by cAMP and probable inhibition of adenylate cyclase in 5-HT nerve terminals by presynaptic α2-adrenoceptors. Naunyn-Schmiedeberg’s Arch. Pharmacol., 336, 251–256

    Google Scholar 

  • Schlicker, E., Classen, K. and Göthert, M. (1988). Presynaptic serotonin receptors and α2-adrenoceptors on central serotoninergic and noradrenergic neurones of normotensive and spontaneously hypertensive rats. J. Cardiovasc. Pharmacol., 11, 518–528

    Google Scholar 

  • Sprouse, J. S. and Aghajanian, G. K. (1986). (−)-Propranolol blocks the inhibition of serotonergic dorsal raphe cell firing by 5-HT1A selective agonists. Eur. J. Pharmacol., 128, 295–298

    Google Scholar 

  • Verbeuren, T. J., Coen, E. P., Schoups. A., van de Velde, R., Baeyens, R. and de Potter, W. P. (1984). Presynaptic serotonin receptors regulate the release of [3H]-serotonin in hypothalamic slices of the rabbit. Naunyn-Schmiedeberg’s Arch. Pharmacol., 327, 102–106

    Google Scholar 

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Göthert, M. (1989). 5-HT Receptors Mediating Pre-synaptic Autoinhibition in Central Serotoninergic Nerve Terminals. 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_7

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