elzasonan

Elzasonan is a selective antagonist of the serotonin 5-hydroxytryptamine 1B receptor and serotonin 5-hydroxytryptamine 1D receptor. It was developed by Pfizer for the treatment of depression and other affective disorders but its development was discontinued due to lack of efficacy. By preferentially blocking presynaptic 5‑HT₁B and 5‑HT₁D autoreceptors, elzasonan is thought to enhance serotonergic neurotransmission from the raphe nucleus to limbic regions such as the hippocampus and prefrontal cortex. This mechanism was hypothesized to produce antidepressant effects. Elzasonan is administered orally and undergoes extensive hepatic metabolism primarily via oxidative N-demethylation, N‑oxidation, aryl hydroxylation (mainly by CYP3A4), with fecal excretion as the main elimination route[1][7][6][4].

Other names

elzasonan hydrochloride(2z)-4-(3,4-dichlorphenyl)-2-(2-(4-methylpiperazin-1-yl)benzylidene)thiomorpholin-3-one3-thiomorpholinone, 4-(3,4-dichlorphenyl)-2-((2-(4-methyl-1-piperazinyl) phenyl)methylene)-, (2z)-