Add time:07/25/2019         Source:sciencedirect.com

4-(p-Bromophenyl)-bicyclo (2,2,2)octan-1-amine was a potent antagonist of p-chloroamphe-tamine-induced depletion of brain serotonin and a weaker antagonist of 6-hydroxydopamine-induced depletion of heart norepinephrine in rats and in mice. In both species, this compound was more active in antagonizing serotonin depletion and less active in antagonizing norepinephrine depletion than was the parent compound lacking the p-bromo substituent. In vitro, the bromo analogue was markedly less active than the parent compound in blocking norepinephrine uptake by rat brain synaptosomes and was slightly less active in blocking serotonin uptake. Brain levels of the p-bromo compound were higher than those of the parent compound in rats, apparently accounting for the relatively greater effectiveness of the f-bromo compound in blocking serotonin depeletion in vivo. Thus, 4-(p-bromophenyl)-bicyclo (2,2,2,)octan-1-amine appears to be a potent and relatively selective inhibitor of uptake into serotonin neurones.

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