Drug intelligence / Profile preview

amoxapine

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Amoxapine is a tricyclic antidepressant (TCA) of the dibenzoxazepine class, primarily used to treat depression, including neurotic or reactive depressive disorders and endogenous or psychotic depression. It is the N-demethylated derivative of loxapine. Amoxapine acts by inhibiting the reuptake of norepinephrine and serotonin in the central nervous system, thereby increasing their levels in the brain. It also antagonizes several neurotransmitter receptors including dopamine D2, serotonin 5‑HT2A/2B/2C/3/6/7, histamine H1, alpha‑1 adrenergic receptors, and muscarinic acetylcholine receptors. These actions contribute to its antidepressant effects as well as side effects such as sedation and anticholinergic symptoms. Its major active metabolites further contribute to its pharmacological profile; for example, 7-hydroxyamoxapine has stronger dopamine receptor antagonism[3][4][8].

Brand names
AsendinAdisenAmolifeAmoxanAsendisDéfanylDemoloxOxamineOxcap
Other names
2-Chloro-11-(1-piperazinyl)dibenz[b,f][1,4]oxazepine
02

Targets

SERT (Sodium-dependent serotonin transporter)HRH1 (Histamine H1 Receptor)HTR2A (Serotonin receptor 5-HT2A)NET (Norepinephrine Transporter)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)

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