Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design of Molecules Acting on the Serotonin Receptors

Author(s): Carmela Saturnino, Mariafrancesca Buonerba, Anna Capasso.

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

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Article Details

VOLUME: 4
ISSUE: 5
Year: 2007
Page: [365 - 367]
Pages: 3
DOI: 10.2174/157018007780867861
Price: $58