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Mirtazapine 5-HT Receptor antagonist

Cat.No.S2016

Mirtazapine (Org3770,6-Azamianserin) is an adrenergic and seroton receptor antagonist, used to treat depression.
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Quality Control

Batch: S201601 DMSO]53 mg/mL]false]Ethanol]53 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 53 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 265.35 Formula

C17H19N3

Storage (From the date of receipt)
CAS No. 85650-52-8 Download SDF Storage of Stock Solutions

Synonyms Org3770,6-Azamianserin SMILES CN1CCN2C(C1)C3=CC=CC=C3CC4=C2N=CC=C4

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Mechanism of Action

Targets/IC50/Ki
5-HT
In vitro

Mirtazapine displays marked affinity for cloned, human alpha2A-adrenergic (AR) receptors at which it blocks noradrenaline (NA)-induced stimulation of guanosine-5'-O-(3-[35S]thio)-triphosphate ([35S]-GTPgammaS) binding. This compound shows high affinity for cloned, human serotonin (5-HT)2C receptors at which it abolishes 5-HT-induced phosphoinositide generation. It markedly elevates dialysate levels of NA and, in FCX, DA, whereas 5-HT is not affected. This chemical enhances the effectiveness of the electrical stimulation of the ascending 5-HT pathway by blocking both alpha-2 adrenergic auto- and heteroreceptors. It blocks the suppressant effect of microiontophoretically applied norepinephrine (NE) on the firing activity of CA3 dorsal hippocampus pyramidal neurons, indicating their antagonistic effects on postsynaptic alpha-2 adrenoceptors.

In vivo

Mirtazapine (10-250 mg/kg i.v.) enhances dose-dependently the firing activity of the 5-HT neurons in naive rats, but not in 6-hydroxydopamine-pretreated rats. This compound (5 mg/kg/day, s.c., using osmotic minipumps) increases the spontaneous firing activity of locus coeruleus noradrenaline (NA) neurons in male Sprague-Dawley rats. It antagonizes both the enhancing effect of a low dose (10 mg/kg, i.v.) and the reducing effect of a high dose (100 mg/kg, i.v.) of the alpha 2-adrenoceptor agonist clonidine on the effectiveness of the electrical stimulation of the ascending 5-HT pathway in suppressing the firing activity of dorsal hippocampus CA3 pyramidal neurons. This chemical (5 mg/kg s.c.) only slightly affects DOPAC and homovanillic acid levels in the striatum, hardly affects 5-HT release in freely moving rats, but clearly increased 5-hydroxyindole acetic acid.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8627567/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-09-24)

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