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GPCR/G Protein 5-HT Receptor Mirtazapine

Mirtazapine

Catalog No. T0137   CAS 85650-52-8
Synonyms: 6-Azamianserin, Org3770
Purity 99.71% Datasheet MSDS

Mirtazapine is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Mirtazapine, CAS 85650-52-8
Pack Size Availability Price/USD Quantity
10 mg Inquiry 60.00
25 mg In stock 108.00
100 mg Inquiry 180.00
200 mg Inquiry 310.00
1 mL * 10 mM (in DMSO) Inquiry 71.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mirtazapine is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.
Targets&IC50 5-HT,   Adrenergic Receptor,   DA transporter,   Dopamine,   HT,   Sert (Sodium-dependent),   κ-opioid receptor,  
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.[1] 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. [2]
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. [2] 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. [3] 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. [4]
Synonyms 6-Azamianserin, Org3770
Purity 99.71%
Appearance solid
Molecular Weight 265.35
Formula C17H19N3
CAS No. 85650-52-8

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

Ethanol: 53 mg/mL (199.73 mM)

DMSO: 53 mg/mL (199.73 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Millan MJ, et al. Eur J Neurosci, 2000, 12(3), 1079-1095. 2. Garcia-Effron G, et al. J Antimicrob Chemother, 2004, 53(6), 1086-1089. 3. Haddjeri N, et al. Naunyn Schmiedebergs Arch Pharmacol, 1997, 355(1), 20-29. 4. de Boer TH, et al. J Pharmacol Exp Ther, 1996, 277(2), 852-860.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Adrenergic Receptor Compound Library Neuronal Signaling Compound Library Endocrinology-Hormones Library Histamine & Melatonin Library Serotonin Compound Library Hematopoietic Toxicity Compound Library FDA-approved Drug Library GPCR Compound Library Anti-Cardiovascular Disease Compound Library CNS-Penetrant Compound Library

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