product name Mianserin HCl
Description: Mianserin HCl (also known as ORG GB-94 HCl), a tetracyclic compound, is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, it is used for the treatment of depression. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.
References: J Pharmacol Exp Ther. 1996 May;277(2):852-60; Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.
300.83
Formula
C18H20N2·HCl
CAS No.
21535-47-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (199.4 mM)
Water: 30 mg/mL (99.7 mM)
Ethanol: 21 mg/mL (69.8 mM)
Solubility (In vivo)
Synonyms
ORG GB-94 HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426923
| In Vitro |
In vitro activity: Mianserin (2 mg/kg s.c.) causes a modest increase of DOPAC levels up to about 30% above base-line, which is statistically significant when compared to saline. Mianserin increases extracellular norepinephnne, but a comparison with desipramine and idazoxan showed that both NE reuptake inhibition and alpha-2 autoreceptor blockade contributed to the mianserin-induced increase in extracellular norepinephnne. Mianserin and eltoprazine displays opposite effects in the elevated plus-maze: Mianserin induces anxiolytic-like effects, while eltoprazine shows anxiogenic-like ones. Mianserin treatment induces a decrease in the number of these sites, while eltoprazine treatment results in an increase. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mianserin, which has a small or no effect in noradrenaline (NA) reuptake but may enhance release by blocking presynaptic inhibition mediated by alpha 2-adrenoceptors, induced regeneration of catecholamine fibers in the rat cerebral cortex. Mianserin attenuates the effects of both m-CPP and SKF 38393 in neonatal 6-OHDA-lesioned rats, suggesting that DA agonist effects are mediated by 5-HT neurochemical systems. Mianserin (10 mg/kg, SC) dose-dependently increases up to about 6 times extracellular dopamine in the medial prefrontal cortex of the rat. Mianserin also dose-dependently increases extracellular noradrenaline in the prefrontal cortex. |
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| References | J Pharmacol Exp Ther. 1996 May;277(2):852-60; Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31; Neuroreport. 1991 Sep;2(9):525-8. |
