Publisher： Bentham Science Publishers
E-ISSN： 1875-628x|4|5|365-367
ISSN： 1570-1808
Source： Letters in Drug Design & Discovery, Vol.4, Iss.5, 2007-07, pp. : 365-367
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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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