Home Neuronal Signaling 5-HT Receptor modulator Flibanserin

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Flibanserin 5-HT Receptor modulator

Cat.No.S3716

Flibanserin (BIMT-17, BIMT-17-BS) 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 5-HT Receptor modulator Chemical Structure

Chemical Structure

Molecular Weight: 390.40

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Quality Control

Batch: S371601 DMSO]78 mg/mL]false]Ethanol]23 mg/mL]false]Water]Insoluble]false Purity: 99.61%
99.61

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 390.40 Formula

C20H21F3N4O

 Storage (From the date of receipt)
CAS No. 167933-07-5 Download SDF Storage of Stock Solutions

Synonyms BIMT-17, BIMT-17-BS Smiles C1CN(CCN1CCN2C3=CC=CC=C3NC2=O)C4=CC=CC(=C4)C(F)(F)F

Mechanism of Action

Targets/IC50/Ki
5-HT1A
(CHO)
1 nM(Ki)
D4 receptor
(CHO)
4-24 nM(Ki)
5-HT2A
(CHO)
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, this compound behaves as a 5-HT1A agonist, a very weak partial agonist on dopamine D4 receptors, and a 5-HT2A antagonist. It also shows some affinity for human D2L and D3 receptors and rat NE-alpha 1 and 5-HT7 receptors. This chemical 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 it 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, its administration has been shown to lead to brain region-specific decreases in serotonin (5-HT) and increases in dopamine and norepinephrine. This compound's exposure is proportional to dose. The plasma protein binding of this chemical (98% to albumin) is high. Its 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 this compound 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. It is well-tolerated at doses up to 100 mg/day (the highest dose tested in PhaseIII) for 24 weeks.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03707340 Active not recruiting
Breast Cancer|Hyposexual Desire Disorder
Memorial Sloan Kettering Cancer Center
 September 14 2018 --
NCT01188603 Completed
Sexual Dysfunctions Psychological
Sprout Pharmaceuticals Inc
 July 2010 Phase 1
NCT00277914 Completed
Sexual Dysfunctions Psychological
Sprout Pharmaceuticals Inc
 January 2006 Phase 3

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