Lometraline

Lometraline (INN; CP-14,368) is a drug which is an aminotetralin derivative. A structural modification of the investigative neuroleptic pinoxepin, lometraline was originally patented by Pfizer as an antipsychotic, tranquilizer, and antiparkinsonian agent (likely as an anticholinergic). However, it was instead later studied as a potential antidepressant and/or anxiolytic agent, but clinical studies revealed no psychoactivity at the doses used and further investigation was suspended. However, further experimental modifications of the chemical structure of lometraline directly resulted in the discovery of tametraline, a potent inhibitor of the reuptake of dopamine and norepinephrine, which in turn led to the discovery of the now widely popular antidepressant sertraline, which, remarkably, acts contrarily as a selective serotonin reuptake inhibitor (SSRI).