Vilazodone HCl

製品コードS4259 バッチS425902

印刷

化学情報

Chemical Structure Synonyms EMD68843,SB659746A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H27N5O2.HCl
分子量 477.99 CAS No. 163521-08-2
Solubility (25°C)* 体外 DMSO 95 mg/mL (198.74 mM)
Water Insoluble
Ethanol 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Vilazodone HCl(EMD68843,SB659746A) is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.
in vitro

Vilazodone demonstrates an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone displays high affinity (pKi ≥ 9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A receptors. [1]
in vivo

Vilazodone selectively enhances serotonergic output in the prefrontal cortex of rats. Vilazodone demonstrates anxiolytic efficacy through Behavioral evaluations in the ultrasonic vocalization model of anxiety in rats. Vilazodone also shows efficacy but at a single dose only in the forced swim test (a putative model of depression). [1] Vilazodone (1-10 mg/kg p.o.) dose-dependently displaces in vivo [3H]DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio)benzylamine) binding from rat cortex and hippocampus, indicating that vilazodone occupies 5-HT transporters in vivo. Vilazodone (10 mg/kg p.o.) is demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. [2] Vilazodone affects stress potentiation of startle at doses above 5 mg/kg in rats. Vilazodone increases stress elevation of startle at 10 mg/kg in rats. Vilazodone (20 and 40 mg/kg) blocked stress potentiation of startle in rats. Vilazodone increases stress elevation of startle at all doses in rats. [3] vilazodone has no effect on 5-HT efflux at 100 nM but significantly decreases 5-HT efflux at 1 mM in the guinea-pig dorsal raphe nucleus. Vilazodone significantly increases the re-uptake half life for 5-HT in the guinea-pig dorsal raphe nucleus. [4]

プロトコル(参考用のみ)

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：

Spinal Serotonin 1A Receptor Contributes to the Analgesia of Acupoint Catgut Embedding by Inhibiting Phosphorylation of the N-Methyl-d-Aspartate Receptor GluN1 Subunit in Complete Freund's Adjuvant-Induced Inflammatory Pain in Rats [ J Pain, 2019, 20(1):16.e1-16.e16] PubMed: 30102991
DETERMINATION OF VENLAFAXINE, VILAZODONE AND THEIR MAIN ACTIVE METABOLITES IN HUMAN SERUM BY HPLC-DAD AND HPLC-MS. [ Acta Pol Pharm, 2017, 74(3):765-775] PubMed: 29513945

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。