Flibanserin
Based on 3 publication(s) in Google Scholar
Flibanserin (BIMT-17; BIMT-17BS) 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 binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.
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- Pureza : 99.9%
- No. CAS: 167933-07-5
- Fòrmula: C20H21F3N4O
- Peso molecular:390.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Flibanserin
MoreVer todos los productos específicos de isoformas 5-HT Receptor
MoreVer todos los productos específicos de isoformas Dopamine Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
5-HT1A Receptor 1 nM (Ki) |
5-HT2A Receptor 49 nM (Ki) |
dopamine D4 receptors 4-24 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NHSF cell lin
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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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).
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long Evans female rats (225-250 g)[3]
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Dosage:15 mg/kg; 45 mg/kg
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Administration:Oral gavage; twice a day for 22 days
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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.
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Animal Model:Rat pup ultrasonic vocalization model of anxiety[4]
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Dosage:5, 10, 25, and 50 mg/kg
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Administration:Subcutaneous injection
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Result:Reduced ultrasonic vocalizations in rat pups.
Showed effective within 30 min and has no severe locomotor side effects at active doses.
Chemical Information
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No. CAS 167933-07-5
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Appearance Solid
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Peso molecular 390.40
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Fòrmula C20H21F3N4O
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Color White to off-white
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SMILES
O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3
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Synonyms
BIMT-17; BIMT-17BS
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Mol Pharmacol
2023 Nov;104(5):230-238. PMID: 37567783 -
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (128.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[3]. Gelez H, et al. Brain neuronal activation induced by flibanserin treatment in female rats. Psychopharmacology (Berl). 2013 Dec;230(4):639-52. [Content Brief]
[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. [Content Brief]
[5]. Gelman F, et al. Flibanserin for hypoactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL | 64.0369 mL |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.1230 mL | 12.8074 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL | 6.4037 mL | |
| 15 mM | 0.1708 mL | 0.8538 mL | 1.7077 mL | 4.2691 mL | |
| 20 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
| 25 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5615 mL | |
| 30 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1346 mL | |
| 40 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2807 mL | |
| 60 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2561 mL | 0.6404 mL |
Flibanserin Related Classifications
HY-A0095 Related Classifications
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Keywords
- Flibanserin
- 167933-07-5
- BIMT-17
- BIMT-17BS
- BIMT17
- BIMT 17
- 5-HT Receptor
- Dopamine Receptor
- affinity
- neurotransmitter
- hypoactive
- sexual
- desire
- disorder
- antidepressant
- antianxiety
- hypoactive sexual desire disorder
- HSDD
- orally active
- DP1
- DP2
- no cytotoxicity
- NHSF cell line
- prefrontal cortex
- hippocampus
- midbrain
- Inhibitor
- inhibitor
- inhibit