• DOI:10.1007/s002100000295
• Corpus ID: 24189673

The interaction of antidepressant drugs with enteric 5-HT7 receptors

@article{Lucchelli2000TheIO,
  title={The interaction of antidepressant drugs with enteric 5-HT7 receptors},
  author={Adele Lucchelli and Maria Grazia Santagostino-Barbone and G D'agostino and Elisabetta Masoero and Marcello Tonini},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2000},
  volume={362},
  pages={284-289}
}

• A. Lucchelli, M. G. Santagostino-Barbone, +2 authors M. Tonini
• Published 18 August 2000
• Psychology
• Naunyn-Schmiedeberg's Archives of Pharmacology

Abstract. In this study the functional interaction of the antidepressant drugs amitriptyline, mianserin, maprotiline, imipramine, fluoxetine and the putative antidepressant drug flibanserin has been studied on 5-HT7-mediated responses to 5-carboxamidotryptamine (5-CT) in the guinea-pig ileum.5-CT induced a concentration-dependent inhibition of the contractile response to substance P (100 nM). Except for fluoxetine and flibanserin, all the antidepressants antagonized by different degrees the 5-CT inhibitory response with the following rank affinity order: mianserin > maprotiline ≥ imipramine > amitriptyline. Mianserin was the only antidepressant to show a profile of competitive antagonism at 5-HT7 receptors in a tenfold range of concentrations (0.1–1 µM), with an affinity (pA2) value of 8.1±0.6. The antagonism of the other antidepressants was not concentration-dependent (amitriptyline) or was associated with slight or moderate reduction of the maximal 5-CT response (imipramine or maprotiline). The apparent affinity (pKB) values were: amitriptyline, 7.0±0.2; maprotiline, 7.3±0.6; imipramine, 7.2±0.4.Our results show that various antidepressant drugs belonging to different chemical classes behave as antagonists at enteric 5-HT7 receptors through competitive or allosteric mechanisms. This evidence extends our previous findings demonstrating the interaction of antidepressants with other 5-HT receptors, namely 5-HT3 and 5-HT4 receptors.