For research use only.

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.
5-HT1A [2]
D4 receptor [2]
5-HT2A [2]
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].


Animal Research:[3]
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  • Animal Models: Sprague-Dawley rats
  • 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


CAS No. 167933-07-5
Storage powder
in solvent
Synonyms BIMT-17, BIMT-17-BS
Smiles FC(F)(F)C1=CC=CC(=C1)N2CCN(CC2)CCN3C(=O)NC4=C3C=CC=C4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID