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 : GC74179Flibanserin 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。
Sample solution is provided at 25 µL, 10mM.
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.
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。 |
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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。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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