Mirtazapine

Biological Activity

Mirtazapine is an antidepressant agent; potent 5-HT₂, 5-HT₃ and histamine H₁ receptor antagonist and moderately potent α₂-adrenoceptor antagonist (pK_i values are 8.05, ~ 8.1, 9.3 and 6.95 respectively). Enhances noradrenaline (NA) release in rat brain via inhibition of α₂-adrenergic autoreceptors and displays only weak affinity for monoamine transporters (pK_i values are 5.6, < 5 and < 5.1 for inhibition of NA, dopamine and 5-HT uptake respectively). Increases hippocampal NA and 5-HT levels in rats following systemic administration in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, ORG 3770 and its enantiomers.
   de Boer et al.
   Neuropharmacology, 1988;27:399
2. Interaction between enantiomers of mianserin and ORG3770 at 5-HT3 receptors in cultured mouse neuroblastoma cells.
   Kooyman et al.
   Neuropharmacology, 1994;33:501
3. Differences in modulation of noradrenergic and serotonergic transmission by the alpha-2 adrenoceptor antagonists, mirtazepine, mianserin and idazoxan.
   de Boer et al.
   J.Pharmacol.Exp.Ther., 1996;277:852

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