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Current Topics in Pharmacology   Volumes    Volume 7  Issue 2
Abstract
Interaction of serotonin receptors on the raphe nuclei
Claire Roberts
Pages: 263 - 267
Number of pages: 5
Current Topics in Pharmacology
Volume 7  Issue 2

Copyright © 2003 Research Trends. All rights reserved

ABSTRACT

The majority of 5-HT fibres originate from the dorsal and median raphe nuclei: DRN and MRN repectively, where 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A and 5-HT7 receptors have been localised in the raphe. Selective receptor antagonists are available to investigate the function of these receptors, except for 5-HT5A where we still await the discovery of selective compounds.

In the DRN, 5-HT1A receptors play an important role in regulating 5-HT release. Both 5-HT1B and 5-HT7 receptor antagonists have little effect on 5-HT release per se but increase 5-HT release in the presence of 5-HT1A receptor blockade. In contrast, 5-HT1D receptor antagonists increase 5-HT release per se and are not affected by 5-HT1A receptor blockade. In the MRN, 5-HT1B receptors are thought to play a more dominant function in regulating 5-HT release. 5-HT1B receptor blockade increases 5-HT release per se which is not modulated by 5-HT1A receptor antagonism.

Therefore, to achieve maximum elevation of 5-HT release in the raphe nuclei one would need either a combination 5-HT1A and 5-HT1B or 5-HT1A and 5-HT7 receptor blockade. However, we await the emergence of selective 5-HT5A compounds to assess the functional importance of this receptor in the raphe.

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