Bioactivity | Bupivacaine hydrochloride 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 hydrochloride can be used for the research of chronic pain[1][2][3]. |
Target | Sodium Channel |
Invitro | Bupivacaine hydrochloride inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization[1]. Bupivacaine hydrochloride 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 hydrochloride IC50=2.18±0.16 μM[2]. Bupivacaine hydrochloride reversibly inhibits the SK2 channel in a dose-dependent manner with the IC 50 of 16.5 µM[3]. Cell Viability Assay[3] Cell Line: |
Name | Bupivacaine hydrochloride |
CAS | 18010-40-7 |
Formula | C18H29ClN2O |
Molar Mass | 324.89 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
Reference | [1]. Casati A, et, al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):247-68. [2]. Dan J, et, al. Inhibition of gastric cancer by local anesthetic bupivacaine through multiple mechanisms independent of sodium channel blockade. Biomed Pharmacother. 2018 Jul;103:823-828. |