Bupivacaine is aNMDA receptorinhibitor.Bupivacaine can blocksodium,L-calcium, andpotassium channels.Bupivacaine potently blocksSCN5A channelswith theIC₅₀of 69.5 μM. Bupivacaine 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 IC₅₀of 16.5 μM^[3].

288.43

Solid

C₁₈H₂₈N₂O

38396-39-3

布比卡因

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