Bupivacaine | 丁吡卡因

MCE 国际站：Bupivacaine

中文名：丁吡卡因

CAS：38396-39-3

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：布比卡因是一种NMDA受体抑制剂。布比卡因可阻断钠、L-钙和钾通道。布比卡因有效阻断 SCN5A 通道，IC₅₀ 为 69.5 μM。布比卡因可用于慢性疼痛的研究^[1][2][3]。 

体外：布比卡因抑制脊髓背角中 NMDA 受体介导的突触传递，脊髓背角是一个与中枢敏化密切相关的区域^[1]。Bupivacaine 通过将半数最大激活/失活的膜电位向稍微更负的膜电位移动来影响通道激活和稳态失活的电压依赖性。在失活状态下，SCN5A 通道对布比卡因 IC₅₀=2.18±0.16 μM^[2] 略微敏感。Bupivacaine 以剂量依赖的方式可逆地抑制 SK2 通道，IC ₅₀ 为 16.5 µM^[3]。

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研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR  |  Sodium Channel  |  Calcium Channel  |  Potassium Channel

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参考文献：[1]. Meaghan A Paganelli, et al. Actions of Bupivacaine, a widely used local anesthetic, on NMDA receptor responses. J Neurosci. 2015 Jan 14;35(2):831-42.

[2]. Alexander P Schwoerer, et al. A Comparative Analysis of Bupivacaine and Ropivacaine Effects on Human Cardiac SCN5A Channels. Anesth Analg. 2015 Jun;120(6):1226-34.

[3]. Carsten Stoetzer, et al. Inhibition of Voltage-Gated Na⁺ Channels by Bupivacaine Is Enhanced by the Adjuvants Buprenorphine, Ketamine, and Clonidine. Reg Anesth Pain Med.Jul/Aug 2017;42(4):462-468.