Flibanserin (BIMT-17; BIMT-17BS) 是一种具有口服活性的 5- 羟色胺的5-HT1A受体激动剂和5-HT2A受体拮抗剂，结合亲和力Ki分别为 1 nM 和 49 nM。Flibanserin 也能够结合多巴胺 D4 受体，Ki为 4-24 nM。Flibanserin 具有抗抑郁和抗焦虑作用，可用于性欲减退 (HSDD) 的研究。
| 生物活性 | Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin5-HT1A receptoragonist and5-HT2A receptorantagonist withKivalues of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with anKivalue of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research[1]-[5]. |
| IC50& Target[2] | 5-HT1AReceptor 1 nM (Ki) | 5-HT2AReceptor 49 nM (Ki) | dopamine D4 receptors 4-24 nM (Ki) |
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体外研究
(In Vitro) | Flibanserin (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation[1].
Cell Viability Assay[1] | Cell Line: | NHSF cell lin | | Concentration: | 0.01, 0.1, 1, 10, 100 μM | | Incubation Time: | 72 hours | | Result: | Resulted cell viability reached to 97.91% (DP1) and 96.73% (DP2) at 0.01 μM.
Showed non-toxic up to 100 μM (IC50>100 μM). |
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体内研究
(In Vivo) | Flibanserin (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 (15, 45 mg/kg; p.o.; twice a day; 22 d) preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and hypothalamic structures involved in the integration of sexual cues related to sexual motivation[3].
Flibanserin (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model[4].
| Animal Model: | Long Evans female rats (225-250 g)[3] | | Dosage: | 15 mg/kg; 45 mg/kg | | Administration: | Oral gavage; twice a day for 22 days | | Result: | Increased the density of activated catecholaminergic neurons in the ventral tegmental area but not in the locus coeruleus.
Increased Fos expression in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus with chronic 22-day treatment. |
| Animal Model: | Rat pup ultrasonic vocalization model of anxiety[4] | | Dosage: | 5, 10, 25, and 50 mg/kg | | Administration: | Subcutaneous injection | | Result: | Reduced ultrasonic vocalizations in rat pups.
Showed effective within 30 min and has no severe locomotor side effects at active doses. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(128.07 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL | | 5 mM | 0.5123 mL | 2.5615 mL | 5.1230 mL | | 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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