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Flibanserin hydrochloride (propan-2-ol) hydrate

(Synonyms: 盐酸氟立班丝氨; BIMT-17 hydrochloride (propan-2-ol) hydrate; BIMT-17BS hydrochloride (propan-2-ol) hydrate) 目录号 : GC74179

Flibanserin hydrochloride (propan-2-ol) hydrateKi值分别为1nM和49nM的口服活性血清素5-HT1A受体激动剂和5-HT2A受体拮抗剂。

Flibanserin hydrochloride (propan-2-ol) hydrate Chemical Structure

规格 价格 库存 购买数量
5 mg
¥405.00
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10 mg
¥675.00
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25 mg
¥1,350.00
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50 mg
¥2,160.00
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100 mg
¥3,420.00
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Sample solution is provided at 25 µL, 10mM.

Description

Flibanserin (drochloride) (propan-2-ol) (drate) (BIMT-17 (drochloride) (propan-2-ol) (drate); BIMT-17BS (drochloride) (propan-2-ol) (drate))is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin drochloride binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin drochloride shows anti-depression and anti-anxiety effect, can be used to poactive sexual desire disorder (HSDD) research-.

Flibanserin (drochloride) (propan-2-ol) (drate) (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation[1].

Flibanserin drochloride (1, 10, 30 mg/kg; i.p.; single dose) shows different pharmacological properties in prefrontal cortex, hippocampus and midbrain. The 5-HT1A receptor occupancy in cortex indicates it’s the more sensitive than other brain region[2].Flibanserin drochloride (15, 45 mg/kg; p.o.; twice a day; 22 d) preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and pothalamic structures involved in the integration of sexual cues related to sexual motivation[3].Flibanserin drochloride (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model[4].

References:
[1]. Fayed M, et al. Insights into Flibanserin Oxidative Stress Degradation Pathway: In Silico – In Vitro Toxicity Assessment of Its Degradates[J]. New Journal of Chemistry, 2021. [2]. Invernizzi RW, et al. 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.
[3]. Gelez H, et al. Brain neuronal activation induced by flibanserin treatment in female rats. Psychopharmacology (Berl). 2013 Dec;230(4):639-52.
[4]. Podhorna J, et al. Flibanserin has anxiolytic effects without locomotor side effects in the infant rat ultrasonic vocalization model of anxiety. Br J Pharmacol. 2000 Jun;130(4):739-46.
[5]. Gelman F, et al. Flibanserin for poactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25.

化学性质

Cas No. SDF
别名 盐酸氟立班丝氨; BIMT-17 hydrochloride (propan-2-ol) hydrate; BIMT-17BS hydrochloride (propan-2-ol) hydrate
分子式 C20H22ClF3N4O.0.5C3H8O.0.5H2O 分子量 465.2
溶解度 储存条件 4°C, sealed storage, away from moisture
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1496 mL 10.7481 mL 21.4961 mL
5 mM 0.4299 mL 2.1496 mL 4.2992 mL
10 mM 0.215 mL 1.0748 mL 2.1496 mL
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