Bupivacaine hydrochloride monohydrate  (Synonyms: 布比卡因盐酸盐水合物)

Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain^[1][2][3].

Bupivacaine 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 Bupivacaine 略微敏感 (IC₅₀=2.18±0.16 μM)^[2]。
Bupivacaine 以剂量依赖的方式可逆地抑制 SK2 通道，IC₅₀ 为 16.5 μM^[3]。

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

342.90

C₁₈H₃₁ClN₂O₂

73360-54-0

布比卡因盐酸盐水合物

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]