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Vinpocetine

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Chemical Structure| 42971-09-5 同义名 : 长春西丁 ;Ethyl apovincaminate;Apovincaminic Acid ethyl ester;Vinpocetine, apovincaminic acid ethyl ester, ethyl apovincaminate, AY 27,255, AY-27,255, RGH 4405, RGH4405, RGH-4405, TCV-3B, TCV 3B, TCV3B, Cavinton, Intelectol;RGH-4405;AY 27255
CAS号 : 42971-09-5
货号 : A305598
分子式 : C22H26N2O2
纯度 : 98%
分子量 : 350.454
MDL号 : MFCD00211233
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(14.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 12 mg/mL(34.24 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

PO 0.5% CMC-Na 32 mg/mL suspension

生物活性
靶点

  • Sodium Channel
描述 Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[3]. Vinp inhibits mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB)-dependent inflammatory responses and oxidative damage in which osteoclasts are often involved[4]. In both in vivo and in vitro experiments, vinpocetine can confer protection of rat renal cells by inhibiting the NF-κB signaling pathway and activating the Nrf2/ARE signaling pathway[5]. Vinpocetine potently suppressed tumor necrosis factor-α-induced nuclear factor kappa-light-chain-enhancer of activated B cells activation and proinflammatory mediator expression in primary cultured macrophages in vitro, as well as in the aorta wall in vivo, suggesting vinpocetine conferred anti-AAA (Abdominal aortic aneurysm) effect at least partially via the inhibition of inflammation[6]. Vinpocetine treatment may exhibit anti-inflammatory activity and alleviate cognitive impairment[7]. The effects of vinpocetine might be attributed not only to its antioxidant and anti-inflammatory properties, but also to its suppressing effect on GSK3β (Glycogen synthase kinase-3β) activity and its downstream BACE1(β-secretase) [8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00719953 - Completed - -
NCT00719953 Elderly Memor... 展开 >>y Impairment 收起 << Phase 4 Completed - Israel ... 展开 >> Suorasky Medical Center Tel-Aviv, Israel 收起 <<
NCT01515839 Traumatic Brain Injury Not Applicable Completed - United States, California ... 展开 >> Amen Clinics, Inc. Newport Beach, California, United States, 92660 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.53mL

5.71mL

2.85mL
参考文献

[1]Zhang F, Yan C, Wei C, Yao Y, Ma X, Gong Z, Liu S, Zang D, Chen J, Shi FD, Hao J. Vinpocetine Inhibits NF-κB-Dependent Inflammation in Acute Ischemic Stroke Patients. Transl Stroke Res. 2017 Jul 9.

[2]Bnczk P, Gulyas B, et al. Role of sodium channel inhibition in neuroprotection: effect of vinpocetine. Brain Res Bull. 2000 Oct;53(3):245-54.

[3]Medina, AE. Vinpocetine as a potent antiinflammatory agent. PNAS. 2010; 107(22): 9921-9922.

[4]Zhu M, Liu H, Sun K, Liu J, Mou Y, Qi D, Zhou C, Abudunaibi M, Tasiken B, Li J, Cheng H, Huang H. Vinpocetine inhibits RANKL-induced osteoclastogenesis and attenuates ovariectomy-induced bone loss. Biomed Pharmacother. 2020 Mar;123:109769

[5]Song W, Yin W, Ding L, Gao Y, Xu J, Yang Y, He X, Gong P, Wei L, Chen W, Zhang J. Vinpocetine reduces cisplatin-induced acute kidney injury through inhibition of NF-κB pathway and activation of Nrf2/ARE pathway in rats. Int Urol Nephrol. 2020 Jul;52(7):1389-1401

[6]Zhang C, Hsu CG, Mohan A, Shi H, Li D, Yan C. Vinpocetine protects against the development of experimental abdominal aortic aneurysms. Clin Sci (Lond). 2020 Nov 27;134(22):2959-2976

[7]Ping Z, Xiaomu W, Xufang X, Liang S. Vinpocetine regulates levels of circulating TLRs in Parkinson's disease patients. Neurol Sci. 2019 Jan;40(1):113-120

[8]Ali AA, Ahmed HI, Khaleel SA, Abu-Elfotuh K. Vinpocetine mitigates aluminum-induced cognitive impairment in socially isolated rats. Physiol Behav. 2019 Sep 1;208:112571