| Description | Bupivacaine (AH-250) 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. |
| In vitro | 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]. |
| Synonyms | AH 250, AH-250, AH250, Bupivacaina, Exparel, Anekain |
| molecular weight | 288.43 |
| Molecular formula | C18H28N2O |
| CAS | 38396-39-3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (86.69 mM) |
| References | 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. 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. 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. |