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Subclassification of presynaptic 5-HT autoreceptors in the human cerebral cortex as 5-HT1Dβ receptors

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Abstract

Human cerebral cortical synaptosomes were used to determine the 5-hydroxytryptamine (5-HT) receptor subtype to which the inhibitory presynaptic 5-HT autoreceptor belongs. The synaptosomes preincubated with [3H]5-HT were superfused and tritium overflow was stimulated by high K+. The K+-evoked tritium overflow, which was Ca2+-dependent but tetrodotoxin-resistant, was concentration-dependently inhibited by the nonselective 5-HTlD1Dα/1Dβ receptor agonist, 5-carboxamidotryptamine. Ketanserin at a concentration which should block the 5-HT1Dα but not the 5-HT1Dβ receptor failed to antagonize the inhibitory effect of 5-carboxamidotryptamine. In contrast, the non-selective 5-HT1Dα/1Dβ receptor antagonist, methiothepin, at a concentration which should block both the 5-HT1Dα and the 5-HT1Dβ receptor abolished the effect of 5-carboxamidotryptamine. It is concluded that the presynaptic 5-HT autoreceptor, which has previously been classified as 5-HT1D, belongs to the 5-HT1Dβ subtype.

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Authors and Affiliations

  1. Institut für Pharmakologie und Toxikologie der Universität Bonn, Reuterstrasse 2b, D-53113, Bonn, Germany

    K. Fink & M. Göthert

  2. Neurochirurgische Klinik der Universität Bonn, Sigmund-Freud-Strasse 25, D-53105, Bonn, Germany

    J. Zentner

Authors
  1. K. Fink
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  2. M. Göthert
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  3. J. Zentner
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Fink, K., Göthert, M. & Zentner, J. Subclassification of presynaptic 5-HT autoreceptors in the human cerebral cortex as 5-HT1Dβ receptors. Naunyn-Schmiedeberg's Arch Pharmacol 352, 451–454 (1995). https://doi.org/10.1007/BF00172785

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  • DOI: https://doi.org/10.1007/BF00172785

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