Drug intelligence / Profile preview

mianserin hydrochloride

Development stage
Unknown
Lead developer
Organon
Modality
Small Molecules
Administration
Oral
01

Overview

Mianserin hydrochloride is a tetracyclic antidepressant (TeCA) belonging to the piperazino-azepine group. Unlike traditional tricyclic antidepressants or SSRIs, it does not significantly inhibit the reuptake of serotonin or norepinephrine. Its primary therapeutic effect is mediated through the blockade of presynaptic alpha-2 adrenergic receptors, which enhances noradrenergic neurotransmission by increasing the release of norepinephrine. Additionally, it acts as a potent antagonist at 5-HT2A, 5-HT2C, 5-HT3, and 5-HT7 serotonin receptors, as well as the H1 histamine receptor. The H1 antagonism is responsible for its significant sedative properties, making it useful for depressed patients with insomnia. Originally developed by Organon and marketed under brand names like Tetramide and Tolvon, it is approved in many countries for the treatment of depressive disorders, although it was never introduced in the United States due to concerns regarding agranulocytosis.

Brand names
TetramideTolvonBolvidonNorvalLantanon
Other names
mianserin hydrochloridemianserin HCl
02

Targets

ADRA1A (α1A)HTR3A (5-hydroxytryptamine receptor 3A)HRH1 (Histamine H1 Receptor)HTR2A (Serotonin receptor 5-HT2A)ADRA2A (α2A)HTR7 (5-hydroxytryptamine receptor 7)HTR2C (5-hydroxytryptamine 2C receptor)ADRA2C (α2C)

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