Flibanserin

Catalog No.S3716 Synonyms: BIMT-17, BIMT-17-BS

Flibanserin Chemical Structure

Molecular Weight(MW): 390.40

Flibanserin is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.

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Biological Activity

Description Flibanserin is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.
Targets
5-HT1A [2]
(CHO)
D4 receptor [2]
(CHO)
5-HT2A [2]
(CHO)
1 nM(Ki) 4-24 nM(Ki) 49 nM(Ki)
In vitro

Flibanserin has preferential affinity for serotonin 5-HT1A, dopamine D4, and serotonin 5-HT2A receptors. In vitro and in microiontophoresis, flibanserin behaves as a 5-HT1A agonist, a very weak partial agonist on dopamine D4 receptors, and a 5-HT2A antagonist. Flibanserin also shows some affinity for human D2L and D3 receptors and rat NE-alpha 1 and 5-HT7 receptors. Flibanserin has different affinity for rat (> 10,000 nM) and human (305-785 nM) D2 receptors. The affinity for all other receptors, including the 5-HT transporter, varies from low to very low[2]. In vitro studies showed that flibanserin reduced forskolin-stimulated cAMP formation in cells and rat tissues and antagonized the accumulation of phosphatidyl inositol turnover induced by 5-HT in the mouse cortex[3].

In vivo In vivo flibanserin binds equally to 5-HT1A and 5-HT2A receptors[2]. In rats, flibanserin administration has been shown to lead to brain region-specific decreases in serotonin (5-HT) and increases in dopamine and norepinephrine. Flibanserin exposure is proportional to dose. The plasma protein binding of flibanserin (98% to albumin) is high. Flibanserin administration leads to brain region-specific increases in dopamine and norepinephrine (which are involved in the ‘excitement’ phase of the sexual response) and decreases in serotonin (5-HT) (which is involved in the ‘inhibitory’ phase). The absolute bioavailability of flibanserin after oral administration is 33.2%, and it is moderately distributed in body tissues, with a half-life of about 10 h. Steady state is established within 3 days. Flibanserin is well-tolerated at doses up to 100 mg/day (the highest dose tested in PhaseIII) for 24 weeks[1].

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: 250 ml/L polyethylene glycol-400 and 22.7 ml/L 1M HCl
  • Dosages: 3 and 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.79 mM)
Ethanol 23 mg/mL (58.91 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.40
Formula

C20H21F3N4O

CAS No. 167933-07-5
Storage powder
in solvent
Synonyms BIMT-17, BIMT-17-BS

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03707340 Recruiting Breast Cancer|Hyposexual Desire Disorder Memorial Sloan Kettering Cancer Center September 14 2018 --
NCT03707340 Recruiting Breast Cancer|Hyposexual Desire Disorder Memorial Sloan Kettering Cancer Center September 14 2018 --
NCT02714049 Terminated Hypoactive Sexual Desire Disorder San Diego Sexual Medicine January 25 2017 Phase 4
NCT02714049 Terminated Hypoactive Sexual Desire Disorder San Diego Sexual Medicine January 25 2017 Phase 4
NCT02770768 Recruiting Hypoactive Sexual Desire Disorder University of Chicago October 2016 Not Applicable
NCT02770768 Recruiting Hypoactive Sexual Desire Disorder University of Chicago October 2016 Not Applicable

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID