Mianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
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Mianserin HCl Mianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors , used for the treatment of depression. In vitro
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.
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. Cell Data
cell lines：LC2/ad cells,\u3000MZ-CRC-1 cells and TT cells
