Flibanserin

製品コードS3716 バッチS371601

印刷

化学情報

Chemical Structure Synonyms BIMT-17, BIMT-17-BS Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H21F3N4O
分子量 390.40 CAS No. 167933-07-5
Solubility (25°C)* 体外 DMSO 78 mg/mL (199.79 mM)
Ethanol 23 mg/mL (58.91 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Flibanserin (BIMT-17, BIMT-17-BS) は、非ホルモン性の中枢作用分子であり、シナプス後5-HT1A受容体のアゴニストとして、また5-HT2A受容体のアンタゴニストとして作用します。
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.

プロトコル(参考用のみ)

動物実験 動物モデル Sprague-Dawley rats
投薬量 3 and 10 mg/kg
投与方法 i.p.

参考

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation [ Arch Biochem Biophys, 2024, 754:109958] PubMed: 38499054
FBXL2 counteracts Grp94 to destabilize EGFR and inhibit EGFR-driven NSCLC growth [ Nat Commun, 2021, 12(1):5919] PubMed: 34635651

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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