Bupivacaine 是一种 NMDA 受体抑制剂。Bupivacaine 可以阻断钠、L-钙和钾通道。Bupivacaine 有效阻断 SCN5A 通道，IC50 为 69.5 μM。Bupivacaine 可用于慢性疼痛的研究。

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

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].

38396-39-3

C18H28N2O

288.43

AH 250;AH-250;Exparel;Anekain;AH250;Bupivacaina

DMSO:25 mg/mL(86.69mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years