Catalog No.S3716 Synonyms: BIMT-17, BIMT-17-BS
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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|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.|
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. 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.
|In vivo||In vivo flibanserin binds equally to 5-HT1A and 5-HT2A receptors. 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.|
|In vitro||DMSO||78 mg/mL (199.79 mM)|
|Ethanol||23 mg/mL (58.91 mM)|
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