Abstract
The existence and function of the presynaptic serotonin (5-HT) autoreceptor has been demonstrated in slices and synaptosomes prepared from various regions of the CNS. 5-HT itself or other 5-HT receptor agonists inhibit the release of 3H-5-HT. This effect is competitively antagonized by certain 5- HT receptor antagonists (such as metitepine), which given alone increase 5-HT release by preventing endogenous 5-HT from activating the autoreceptor. In the rat, the presynaptic autoreceptor conforms to the characteristics of the 5-HT1B binding sites (which, however, only occur in this species and the mouse) and, hence, differs from the soma-dendritic (5-HT1A) autoreceptor. Recently, a new subtype of 5-HT1 binding sites termed 5-HT1D was found in, e.g., the porcine and human brain, and evidence has now been obtained in our laboratory that in the pig brain cortex this site is involved in the presynaptic autoregulation of 5-HT release. 5-HT1D receptors also inhibit adenylate cyclase in the brain. The potencies of 5-HT receptor agonists in producing this effect and in inhibiting 5-HT release in the pig brain cortex were correlated, suggesting that the autoreceptor may be negatively coupled to adenylate cyclase.
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© 1990 Kluwer Academic Publishers
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Göthert, M., Sghlicker, E. (1990). Modulation of Serotonin Release in the Central Nervous System via Presynaptic 5-HT Autoreceptors. In: Paoletti, R., Vanhoutte, P.M., Brunello, N., Maggi, F.M. (eds) Serotonin. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-1912-9_38
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DOI: https://doi.org/10.1007/978-94-009-1912-9_38
Publisher Name: Springer, Dordrecht
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