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MCE 国际站:Vortioxetine
中文名:沃替西汀
CAS:508233-74-7
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:Vortioxetine 是 5-HT1A、5-HT1B、5-HT3A、5-HT 的抑制剂7 受体和 SERT,Ki 值为 15 nM、33 nM、3.7 nM、19 nM和 1.6 nM,分别。 IC50 和目标:Ki:15 nM (5-HT1A); 33 nM (5-HT1B); 3.7 nM (5-HT3A); 19 nM (5-HT7); 1.6 纳米 (SERT)[1]。
体外:Vortioxetine (Compound 5m) 是一种多模式血清素能药物,抑制 5-HT1A, 5-HT1B, 5-HT3A, 5- HT7 受体和 SERT,Ki 值分别为 15 nM、33 nM、3.7 nM、19 nM 和 1.6 nM。 Vortioxetine 在 5-HT3A 和 5-HT7 受体上表现出拮抗特性,在 5-HT1B 受体上表现出部分激动剂特性,在5-HT1A 受体,并有效抑制 SERT[1]。 Vortioxetine 是一种部分 h5-HT1B 受体激动剂,EC50 为 460 nM,使用基于全细胞 cAMP 的测定时,内在活性为 22%。 Vortioxetine 与 r5-HT7 受体结合,Ki 值为 200 nM,是 r5-HT7 受体的功能性拮抗剂在体外全细胞 cAMP 测定[5] 中,IC50 为 2 μM。
体内:Vortioxetine (Lu AA21004) 在皮下给药后占据 r5-HT1B 受体和 rSERT(ED50= 3.2 和 0.4 mg/kg,分别),是一种 5-HT 3受体拮抗剂[6]。治疗 21 天后,Vortioxetine 显着增加细胞增殖和细胞存活,并刺激海马齿状回亚颗粒区未成熟颗粒细胞的成熟[3]。沃替西汀不会引起认知或精神运动障碍[4]。
热销产品:EZ-482 | Theaflavin-3'-gallate | NecroX-5 | AA147 | 2-Thenoyltrifluoroacetone | Nalidixic acid | SC144 | Citral | MRK-016 | Zingiberene
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor | Serotonin Transporter
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Bang-Andersen B, Ruhland T, J?rgensen M, Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21.
[2]. Guilloux JP, Mendez-David I, Pehrson A, Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 May 28;73C:147-159.
[3]. Theunissen EL, Street D, H?jer AM, A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013 Jun;93(6):493-501.
[4]. Rothschild AJ, Mahableshwarkar AR, Jacobsen P, Vortioxetine (Lu AA21004) 5mg in generalized anxiety disorder: results of an 8-week randomized, double-blind, placebo-controlled clinical trial in the United States. Eur Neuropsychopharmacol. 2012 Dec;22(12):858-66.
[5]. M?rk A, Pehrson A, Brennum LT, Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J Pharmacol Exp Ther. 2012 Mar;340(3):666-75.
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