mianserin

Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.

Mianserin-d3 is a deuterated compound of Mianserin. Mianserin has a CAS number of 24219-97-4. Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

Mianserin-d3 HCl is a deuterated compound of Mianserin HCl. Mianserin HCl has a CAS number of 21535-47-7. Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.