Effects of 2-substituted-4-phenylquinolines on uptake of serotonin and norepinephrine by isolated brain synaptosomes |
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Authors: | A A Alhaider E J Lien R W Ransom M B Bolger |
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Institution: | Section of Biomedical Chemistry, School of Pharmacy, University of Southern California, Los Angeles, California 90033, USA |
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Abstract: | In this present communication, the in vitro inhibition of the uptake of 3H]-L-norepinephrine (3H] NE) and 3H]-Serotonin (3H] 5-HT) by eleven synthesized 2-substituted-4-phenyl quinolines were studied using rat brain synaptosomal preparations. Compounds with an open side chain were relatively weak inhibitors of the synaptosomal uptake of 3H] NE and 3H] 5HT. Compounds having a distance of three atoms between the terminal basic nitrogen of the side chain and the quinoline ring were better inhibitors of serotonin uptake than those compounds having a four-atom distance. The replacement of the side chain with a piperazine ring produced compounds which were more potent and selective inhibitors of the uptake of either 3H] 5-HT or 3H] NE. Further structure-activity relationships are also discussed. |
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