Flibanserin (Synonyms: BIMT 17) |
| Catalog No.GC11100 |
Flibanserin(BIMT-17; BIMT-17BS)은 각각 1nM 및 49nM의 Ki 값을 갖는 경구 활성 세로토닌 5-HT1A 수용체 작용제 및 5-HT2A 수용체 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 167933-07-5
Sample solution is provided at 25 µL, 10mM.
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Flibanserin is a full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A.
Atypical antipsychotic drugs, all of which are relatively more potent as serotonin (5-HT)(2A) than dopamine D(2) antagonists, improve negative symptoms and cognitive dysfunction in schizophrenia partiallly by increasing cortical dopamine release. 5-HT(1A) agonism is also reported to contribute to the ability to increase cortical dopamine release.
In vitro: Previous study found that flibanserin was a 5-HT(1A) agonist, a very weak partial agonist on dopamine D(4) receptors, and a 5-HT(2A) antagonist. Flibanserin could reduce neuronal firing rate and flibanserin-induced reduction in firing rate was likely mediated via stimulation of postsynaptic 5-HT(1A) receptors. Moreover, flibanserin could quickly desensitize somatic 5-HT autoreceptors and enhance tonic activation of postsynaptic 5-HT(1A) receptors. In addition, flibanserin was able to reduce synthesis and extracellular levels of 5-HT in the cortex [1].
In vivo: Previous animal study showd that flibanserin had antidepressant-like activity in most animal models sensitive to antidepressants, and such activity seemed different from that exerted by other antidepressants. In addition, flibanserin did not show consistent effects in animal models of anxiety and seemed to exert potential antipsychotic effects [1].
Clinical trial: In premenopausal women with HSDD, flibanserin showed significant improvements in the number of SSE and sexual desire. Flibanserin treatment also led to significant reductions in distress associated with sexual dysfunction and distress associated with low sexual desire [2].
References:
[1] Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S. Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42.
[2] Katz M et al. Efficacy of flibanserin in women with hypoactive sexual desire disorder: results from the BEGONIA trial. J Sex Med. 2013 Jul;10(7):1807-15.
| Cas No. | 167933-07-5 | SDF | |
| Synonyms | BIMT 17 | ||
| Chemical Name | 1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one | ||
| Canonical SMILES | O=C1N(CCN2CCN(C3=CC(C(F)(F)F)=CC=C3)CC2)C4=CC=CC=C4N1 | ||
| Formula | C20H21F3N4O | M.Wt | 390.4 |
| Solubility | ≤15mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.123 mL |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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