Etoperidone

Etoperidone (Axiomin, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and thozalinone, is an antidepressant of the piperazine chemical class which was introduced in 1977, but has since been discontinued.

Etoperidone acts as an antagonist at a number of receptors in the following order of potency: 5-HT2 receptor (36 nM) > α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) > α2-adrenergic receptor (570 nM). It also has weak or negligible affinity for blocking the following receptors: D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > muscarinic acetylcholine receptors (>35,000). Etoperidone has weak affinity for the monoamine transporters as well: serotonin transporter (890 nM) > norepinephrine transporter (20,000) > dopamine transporter (52,000).

Synthesis


Palazzo, G.; 1974,.