氟立班丝氨作用机制 - Medchemexpress - MCE中国

Flibanserin

10% DMSO 40% PEG300 5% Tween-80 45% saline

10% DMSO 90% corn oil

以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。

BIOLOGICAL ACTIVITY

?物活性Flibanserin (BIMT-17) 是 5-羟?胺 (5-HT1A) 受体 (K i=1 nM) 的完全激动剂和 5-HT2A 拮抗剂 (49 nM)。Flibanserin 与多巴胺 D4 受体 (K i=4-24 nM) 结合，对多种其他神经递质受体和离?通道的亲和?可忽略不计。Flibanserin 有效治疗性

欲减退 (HSDD)。

IC?? & Target5-HT1A Receptor

1 nM (Ki)5-HT2A Receptor

49 nM (Ki)

dopamine D4 receptors

4-24 nM (Ki)

体内研究The multifunctional serotonergic agent Flibanserin is both a serotonin 1A agonist and a serotonin 2A antagonist.

Flibanserin theoretically improves sexual functioning by enhancing downstream release of dopamine and

norepinephrine while reducing serotonin release in the brain circuits that mediate symptoms of reduced sexual

interest and desire. Flibanserin, a new molecular entity for the treatment of hypoactive sexual desire disorder (HSDD)

in premenopausal women. Flibanserin improves interest in and desire for sex by hypothetically targeting these circuits

and causing the release of dopamine and norepinephrine while also reducing the release of serotonin. Flibanserin has

demonstrated clinical efficacy in premenopausal women who have reduced interest in and desire for sex and has 2

principal pharmacologic actions in microcircuits: it is a full agonist at postsynaptic serotonin 5HT1A receptors and an

antagonist at postsynaptic 5HT2A receptors.

REFERENCES

[1]. Gelman F, et al. Flibanserin for hypoactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25.

[2]. Invernizzi RW, et al. Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8.

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Caution: Product has not been fully validated for medical applications. For research use only.

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