Abstract
The present study examines the pharmacological profile of a new five indole derivatives 2a-e, ligands of the serotonin receptor evaluating the affinity for the serotoninergic, (5HT1A, 5HT2A and 5HT2C) receptors. The affinity of indole derivatives 2a-e (10-6-5x10-7-10-7 M) for receptors is defined as inhibition percentage of radioligand/receptor binding and measured as the radioactivity of remaining complex radioligand/receptor. The results of our experiments indicate that compounds 2a and 2e show high affinity for the 5-HT2A receptors; compounds 2b and 2c show high affinity for the 5-HT1A receptors and compound 2d shows high affinity for the 5-HT2C receptors. Results of computational chemistry suggest that the presence of a methoxyl group in 6 on the indole system is necessary for the serotoninergic activity.
Keywords: Serotoninegic system, Indole derivatives, Binding studies
Letters in Drug Design & Discovery
Title: Design of Molecules Acting on the Serotonin Receptors
Volume: 4 Issue: 5
Author(s): Carmela Saturnino, Mariafrancesca Buonerba and Anna Capasso
Affiliation:
Keywords: Serotoninegic system, Indole derivatives, Binding studies
Abstract: The present study examines the pharmacological profile of a new five indole derivatives 2a-e, ligands of the serotonin receptor evaluating the affinity for the serotoninergic, (5HT1A, 5HT2A and 5HT2C) receptors. The affinity of indole derivatives 2a-e (10-6-5x10-7-10-7 M) for receptors is defined as inhibition percentage of radioligand/receptor binding and measured as the radioactivity of remaining complex radioligand/receptor. The results of our experiments indicate that compounds 2a and 2e show high affinity for the 5-HT2A receptors; compounds 2b and 2c show high affinity for the 5-HT1A receptors and compound 2d shows high affinity for the 5-HT2C receptors. Results of computational chemistry suggest that the presence of a methoxyl group in 6 on the indole system is necessary for the serotoninergic activity.
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Cite this article as:
Saturnino Carmela, Buonerba Mariafrancesca and Capasso Anna, Design of Molecules Acting on the Serotonin Receptors, Letters in Drug Design & Discovery 2007; 4 (5) . https://dx.doi.org/10.2174/157018007780867861
DOI https://dx.doi.org/10.2174/157018007780867861 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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