Home Neuronal Signaling 5-HT Receptor modulator Flibanserin

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Flibanserin 5-HT Receptor modulator

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

Purity & Quality Control

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

Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Mechanism of Action

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
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[2]. 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[3].

In Vivo
In vivo In vivo flibanserin binds equally to 5-HT1A and 5-HT2A receptors[2]. 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[1].
Animal Research Animal Models Sprague-Dawley rats
Dosages 3 and 10 mg/kg
Administration i.p.
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

References
  • https://pubmed.ncbi.nlm.nih.gov/20887163/
  • https://pubmed.ncbi.nlm.nih.gov/12890707/
  • https://pubmed.ncbi.nlm.nih.gov/12890707/

Chemical Information

Molecular Weight 390.40 Formula

C20H21F3N4O
CAS No. 167933-07-5 SDF Download SDF
Synonyms BIMT-17, BIMT-17-BS
Smiles C1CN(CCN1CCN2C3=CC=CC=C3NC2=O)C4=CC=CC(=C4)C(F)(F)F

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble


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In vivo
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