Novel serotonergic agents.

Abstract

The preliminary structure-activity relationships are described for a series of substituted phenethylamines that induce the release of neuronal serotonin. Structures that also have the ability to release neuronal catecholamines are toxic to serotonin neurons, leading to long-term reductions in serotonin markers in rat brain. Conversely, compounds that are selective for the serotonin uptake carrier, and do not affect catecholamines, are not neurotoxic. It is suggested that these novel, selective serotonin releasing agents may find therapeutic utility in disorders where serotonin uptake inhibitors are currently employed.