5-HT Transporter Inhibitors

5-HT transporters (serotonin transporters, SERT) are sodium- and chloride-dependent members of the solute carrier family 6 (SLC6) found widely distributed throughout the brain. They are responsible for re-uptake of 5-HT and undergo a conformational change to move one or more molecules per cycle.

Structural motifs include 12-TM domains, extracellular loops, cytoplasmic C- and N-termini, putative phosphorylation sites acting as potential targets for PKA and PKC and regions essential for 5-HT selective affinity. There is evidence to suggest that SERTs are linked to neuroticism, sexual behavior, alcoholism, clinical depression, hypertension and obsessive-compulsive disorder.