The dissociation rates of [H-3]nisoxetine, [H-3]GBR 12935 and [H-3]cit
alopram from, respectively, the rat brain noradrenaline, dopamine and
5-HT transporters were found to be markedly affected by several drugs.
Sertraline strongly attenuated the rate of dissociation of [H-3]nisox
etine from the noradrenaline transporter, while citaropram strongly at
tenuated that of [H-3]citalopram from the 5-HT transporter. The effect
s of both drugs were stereospecific. Less potent affinity-modulating d
rugs were identified with regards to [H-3]GBR 12935 dissociation from
the dopamine transporter. All three neuronal monoamine transporters ma
y thus have specific affinity-modulating sites which change the functi
on of the transporters with possible implications for the reuptake of
monoamines released during synaptic activity.