Bupivacaine hydrochloride monohydrate 

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 inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization^[1].
Bupivacaine influences the voltage dependency of channel activation and steady-state inactivation by shifting the membrane potential of half-maximal activation/inactivation toward somewhat more negative membrane potentials. In their inactivated state, SCN5A channels are slightly sensitive toward Bupivacaine IC₅₀=2.18±0.16 μM^[2].
Bupivacaine reversibly inhibits the SK2 channel in a dose-dependent manner with the IC ₅₀ of 16.5 μM^[3].

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

342.90

C₁₈H₃₁ClN₂O₂

73360-54-0

CCCCN1CCCCC1C(=O)NC2=C(C=CC=C2C)C.O.Cl

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]