Bupivacaine hydrochloride 是NMDA受体抑制剂，可用于慢性疼痛的研究。它可阻断钠、L-钙和钾通道，还阻断SCN5A通道，IC50为 69.5 μM。

Bupivacaine Hydrochloride is a long-acting, amide-type local anesthetic. Bupivacaine reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.

Bupivacaine可以诱导大鼠肌质网（SR）的Ca2+释放,并抑制SR对钙的吸收.

体外作用15至30分钟,Bupivacaine对牛关节软骨细胞产生细胞毒性。Bupivacaine作用于分离线粒体,是氧消耗和磷酸二磷酸腺苷的解偶联剂。在分离的线粒体中,Bupivacaine浓度依赖性引起线粒体去极化以及吡啶核苷酸氧化。Bupivacaine导致转换孔的开口（PTP）通透性打开,PTP是一个环孢菌素A敏感内膜通道,对许多形式的细胞死亡起着关键作用。

18010-40-7

C18H29ClN2O

324.89

Bupivacaine HCl;Vivacaine;盐酸布比卡因

H2O:21 mg/mL (64.6 mM)
Ethanol:60 mg/mL (184.7 mM)
DMSO:60 mg/mL (184.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years