Antidepressant Gatekeeper - Structural and functional studies point to tricyclics' mechanism of action

AN IMPORTANT CLASS of drugs-tricyclic antidepressants (TCAs)—binds in a surprising place. That finding, based on studies with a bacterial protein, could influence the design of new drugs for depression.

According to two new studies, TCAs seal off a molecular passageway in a bacterial counterpart of human neurotransmitter transporter proteins (Nature, DOI: 10.1038/nature06038 and Science, DOI: 10.1126/science.1147614). The work indicates a molecular mechanism of action for this compound class.

Since the 1950s, TCAs such as desipramine (Norpramin and Pertofrane) have been prescribed to treat symptoms of depression. They prevent reuptake of serotonin and norepinephrine by binding to corresponding membrane-spanning neurotransmitter transporter proteins

READ MORE @ CHEMICAL & ENGINEERING NEWS