Flibanserin

Catalog No.S3716 Batch:S371601

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Technical Data

Formula

C20H21F3N4O
Molecular Weight 390.40 CAS No. 167933-07-5
Solubility (25°C)* In vitro DMSO 78 mg/mL (199.79 mM)
Ethanol 23 mg/mL (58.91 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
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 (from reference)

Animal Study:[3]
  • Animal Models

    Sprague-Dawley rats

  • Dosages

    3 and 10 mg/kg

  • Administration

    i.p.

Selleck's Flibanserin has been cited by 1 publication

FBXL2 counteracts Grp94 to destabilize EGFR and inhibit EGFR-driven NSCLC growth [ Nat Commun, 2021, 12(1):5919] PubMed: 34635651

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.