Serotonin, dopamine and norepinephrine transporters in the central nervous system and their inhibitors.

An overview is presented on progress made in the research on neuronal transporters of serotonin, dopamine and norepinephrine in the central nervous system. Tools developed by molecular biology, such as expression of cloned transporters, their mutants and chimera in non-neuronal cells offered the opportunity to study the putative domains for binding of substrates and uptake inhibitors and discover factors in the regulation of the transporter function. The study of the distribution of monoamine transporters in human brain became possible by the development of selective radiolabelled transport inhibitors. The relationships between the chemical structure of the uptake inhibitors and the affinity for the monoamine transporters is reported, and the (potential) therapeutic applications of the compounds are discussed.