Description: Potent 5-HT2 antagonist. Also 5-HT3, H1 and α2-antagonist. Antidepressant
Alternative Names: Org 3770, 6-Azamianserin
Chemical Name: 1,2,3,4,10,14b-Hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c][2]benzazepine
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Antidepressant agent; potent 5-HT2, 5-HT3 and histamine H1 receptor antagonist and moderately potent α2-adrenoceptor antagonist (pKi values are 8.05, ~ 8.1, 9.3 and 6.95 respectively). Enhances noradrenalin (NA) release in rat brain via inhibition of α2-adrenergic autoreceptors and displays only weak affinity for monoamine transporters (pKi 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.
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Technical Data
M. Wt
265.36
Formula
C17H19N3
Storage
Store at RT
Purity
≥99% (HPLC)
CAS Number
85650-52-8
PubChem ID
4205
InChI Key
RONZAEMNMFQXRA-UHFFFAOYSA-N
Smiles
CN1CCN2C(C1)C1=CC=CC=C1CC1=C2N=CC=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
5.31
20
ethanol
13.27
50
Preparing Stock Solutions
The following data is based on the product molecular weight 265.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.77 mL
18.84 mL
37.68 mL
5 mM
0.75 mL
3.77 mL
7.54 mL
10 mM
0.38 mL
1.88 mL
3.77 mL
50 mM
0.08 mL
0.38 mL
0.75 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
de Boeret al (1988) Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, ORG 3770 and its enantiomers. Neuropharmacology 27 399 PMID: 3419539
Kooymanet al (1994) Interaction between enantiomers of mianserin and ORG3770 at 5-HT3 receptors in cultured mouse neuroblastoma cells. Neuropharmacology 33 501 PMID: 7984289
de Boeret al (1996) Differences in modulation of noradrenergic and serotonergic transmission by the alpha-2 adrenoceptor antagonists, mirtazepine, mianserin and idazoxan. J.Pharmacol.Exp.Ther. 277 852 PMID: 8627567