STRUCTURE ACTIVITY RELATIONS FOR THE INHIBITION OF 5-HT UPTAKE INTO RAT HYPOTHALAMIC HOMOGENATES BY SEROTONIN AND TRYPTAMINE ANALOGUES |
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| Authors: | A S Horn |
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| Institution: | MRC Neurochemical Pharmacology Unit, Department of Pharmacology, University of Cambridge Medical School, Cambridge, U.K. |
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| Abstract: | Abstract— Various 5-HT and tryptamine analogues have been examined as inhibitors of 3H]5-HT uptake into rat hypothalamic homogenates. Acetylation of the terminal amino group or methylation of the hydroxyl group of 5-HT resulted in compounds having a reduced affinity for the serotonin uptake site. This also occurred when the hydroxyl group of 5-HT was substituted in other positions on the benzene ring. Substitution of the tryptamine side chain in the a-position by methyl or ethyl groups, but not by a carboxyl function, enhanced the affinity for the 5-HT uptake site. Increasing the tryptamine side chain by one carbon atom also resulted in a more potent compound. Several of the compounds tested are known to be either hallucinogens or antidepressants. |
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