Benserazide  (Synonyms: 苄丝肼; Ro 4-4602)

Benserazide is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide is also a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the study of Parkinson's disease and melanoma^[1][2][3].

Benserazide 和左旋多巴 (LD) 单独使用或联合使用（Benserazide + 左旋多巴）（25 μM；0 小时、12 小时、24 小时和 168 小时；SH-SY5Y）治疗可抑制蛋白质聚集，并能够最大限度地降低淀粉样蛋白在人神经母细胞瘤细胞系中诱导的细胞毒性。Benserazide 和 LD 均可有效抑制细胞毒性 HSA 聚集体的形成，同时加入这两种药物时抑制效果更明显^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Benserazide (5-50 mg/kg；腹膜内注射；雄性 Wistar 大鼠) 治疗 6-OHDA 损伤大鼠后，外源性 L-DOPA 来源的细胞外 DA 水平升高，Benserazide 剂量依赖性地延长 DA 达到峰值的时间。失神经支配纹状体组织中的 AADC 活性在 10 mg/kg 和 50 mg/kg Benserazide 作用下明显降低。Benserazide 降低黑质纹状体失神经支配大鼠纹状体中枢 AADC 活性，导致外源性 L-DOPA 代谢改变^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

257.24

C₁₀H₁₅N₃O₅

322-35-0

苄丝肼

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhou Y, et al. Benserazide is a novel inhibitor targeting PKM2 for melanoma treatment. Int J Cancer. 2020 Jul 1;147(1):139-151.  [Content Brief]

  [2]. Shen H, et al. Effects of benserazide on L-DOPA-derived extracellular dopamine levels and aromatic L-amino acid decarboxylase activity in the striatum of 6-hydroxydopamine-lesioned rats. Tohoku J Exp Med. 2003 Mar;199(3):149-59.  [Content Brief]

  [3]. Chandel TI, et al. A multiparametric analysis of the synergistic impact of anti-Parkinson's drugs on the fibrillation of human serum albumin. Biochim Biophys Acta Proteins Proteom. 2019 Mar;1867(3):275-285.  [Content Brief]