Mianserin

Mianserin 是一种 H1 受体反向激动剂，是四环类抗抑郁药的精神活性剂。

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5mg

￥425.00

340.00

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100mg

￥1100.00

880.00

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货号: ajci15278
CAS: 24219-97-4
别名: 米安色林; Mianserine
分子式: C18H20N2
分子量: 264.36
纯度: >98%
溶解度: Soluble in DMSO; >16 mg/mL in DMSO; >50 mg/mL in Methanol with ultrasonic; >10 mg/mL in EtOH with ultrasonic
储存: Store at -20°C
库存: 现货

Background

Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.Target: H1 receptorMianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects. It is not approved for use in the US, but its analogue, mirtazapine, is. Mianserin was the first antidepressant to reach the UK market that was less dangerous than the tricyclic antidepressants in overdose.Mianserin is an antagonist/inverse agonist of the H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, and also inhibits the reuptake of norepinephrine. As a high affinity H1 receptor inverse agonist, mianserin has strong antihistamine effects (sedation, weight gain, etc.). Contrarily, it has negligible affinity for the mACh receptors, and thus lacks any anticholinergic properties. It was recently found to be a potent kappa opioid receptor agonist. In addition, mianserin also appears to be a potent antagonist of the neuronal octopamine receptor. What implications this may have on mood are currently unknown, however octopamine has been implicated in the regulation of sleep, appetite and insulin production and therefore may theoretically contribute to the overall side effect profile of mianserin.

参考文献:
[1]. Olianas MC, et al. The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors. Br J Pharmacol. 2012 Nov;167(6):1329-41.
[2]. Roeder T. High-affinity antagonists of the locust neuronal octopamine receptor. Eur J Pharmacol. 1990 Nov 27;191(2):221-4.