Drug intelligence / Profile preview

etoperidone

Development stage
Discontinued
Lead developer
Angelini
Modality
Small Molecules
Administration
Oral
01

Overview

Etoperidone is an atypical antidepressant of the phenylpiperazine class introduced in Europe in 1977. It is a triazole derivative structurally related to trazodone and nefazodone. Etoperidone acts primarily as an antagonist at serotonin 5-HT2A receptor and α1-adrenergic receptor, with additional activity as a partial agonist at 5-HT1A receptor. It also exhibits weak inhibition of serotonin reuptake and has low affinity for dopamine D2, histamine H1, muscarinic acetylcholine (mACh), norepinephrine transporter (NET), and dopamine transporter (DAT) sites. Its major active metabolite is meta-chlorophenylpiperazine (mCPP), which contributes to its serotonergic effects by acting as an agonist at 5-HT2C and antagonist at 5-HT2A receptors. Etoperidone was studied for depression, tremors in Parkinson's disease, extrapyramidal symptoms, and male impotence but was withdrawn from the market due to poor tolerability at effective doses[1][2][3][4][7].

Brand names
StaffAxiominAntifront
Other names
etoperidone hydrochloride
02

Targets

ADRA1A (α1A)SERT (Sodium-dependent serotonin transporter)HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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