Mechanism by which uptake inhibitors antagonize p-chloroamphetamine-induced depletion of brain serotonin.

The mechanism by which uptake inhibitors antagonize p-chloroamphetamine (PCA)-induced depletion of brain serotonin has been suggested to involve: (1) blockade of PCA uptake into the serotonin neuron by means of the membrane carrier, or (2) blockade of the efflux of released serotonin from the neuron, this efflux also requiring the membrane carrier. According to either mechanism, antagonism of serotonin depletion by PCA would provide a valid index of inhibition of the amine uptake system on serotonin neurons in vivo.