Mirtazapine

SKU: orb1310902

Description

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a unique pharmacological profile. It is used in research to study its mechanisms as a noradrenergic and specific serotonergic antidepressant (NaSSA) in both in vitro receptor binding assays and in vivo behavioral models. The compound has been associated with transient, asymptomatic liver enzyme elevations in clinical use.

Research Area

Immunology & Inflammation, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 85650-52-8
• MW: 265.35
• Purity: 99.98% (May vary between batches)
• Formula: C₁₇H₁₉N₃
• SMILES: CN1CC2N(C=3C(CC=4C2=CC=CC4)=CC=CN3)CC1
• Target: Adrenergic Receptor,5-HT Receptor,Dopamine Receptor,Opioid Receptor,Histamine Receptor
• Solubility: Ethanol:53 mg/mL (199.74 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:62.5 mg/mL (235.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.54 mM)

Bioactivity

• Target IC50:
  H1 Receptor:9.3 (pKi)|5-HT2 receptor:8.05 (pKi)|5-HT3 receptor:8.1 (pKi)|α2-adrenoceptor:6.95 (pKi)
• 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. Mirtazapine (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. Mirtazapine 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. Mirtazapine (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.
• 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. Mirtazapine shows high affinity for cloned, human serotonin (5-HT)2C receptors at which it abolishes 5-HT-induced phosphoinositide generation. Mirtazapine markedly elevates dialysate levels of NA and, in FCX, DA, whereas 5-HT is not affected. Mirtazapine enhances the effectiveness of the electrical stimulation of the ascending 5-HT pathway by blocking both alpha-2 adrenergic auto- and heteroreceptors. Mirtazapine 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Histamine Receptor, HistamineReceptor, HT, oral, Org 3770, Org3770, Org-3770, Opioid Receptor, OpioidReceptor, Mirtazapine, inhibit, Inhibitor, noradrenergic, Beta Receptor, Dopamine, Dopamine Receptor, DopamineReceptor, DA transporter, 5-HT3, 5-HT Receptor, 5-HT2, Adrenergic Receptor, AdrenergicReceptor, 61337-67-5, 5-hydroxytryptamine Receptor, 5HTReceptor, 6-Azamianserin, 5HT Receptor, 5-HT, autoimmune, Antidepressant, α2-adrenoceptor, κ-opioid receptor, TNFα, serotonergic, Serotonin Receptor, Sert (Sodium-dependent)

Compound Identifiers

PubChem CID

4205