Catalog No.S2016 Synonyms: Org3770
Molecular Weight(MW): 265.35
Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.
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Choose Selective 5-HT Receptor Inhibitors
|Description||Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.|
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. 
|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||DMSO||53 mg/mL (199.73 mM)|
|Ethanol||53 mg/mL (199.73 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03785691||Recruiting||Drug: Mirtazapine|Drug: Ondansetron|Drug: Placebo||Hyperemesis Gravidarum|Nausea Gravidarum|Vomiting of Pregnancy||Nordsjaellands Hospital|Bispebjerg Hospital|Aalborg University Hospital|Aarhus University Hospital|Herlev and Gentofte Hospital|Hvidovre University Hospital|Odense University Hospital|Rigshospitalet Denmark|Regionernes Medicinpulje||March 1 2019||Phase 2|
|NCT03935685||Recruiting||Drug: Mirtazapine (Remeron)||Glioma of Brain||University of California Irvine||February 26 2019||Early Phase 1|
|NCT02336750||Recruiting||Drug: Aprepitant|Drug: Mirtazapine||Breast Cancer||Fudan University||December 2014||Phase 3|
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