Title: Design of Molecules Acting on the Serotonin Receptors
VOLUME: 4 ISSUE: 5
Author(s):Carmela Saturnino, Mariafrancesca Buonerba and Anna Capasso
Affiliation:Department of Pharmaceutical Sciences, Via Ponte Don Melillo, 84084 -Fisciano (Salerno) Italy.
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.
