PeptideDB

Bupivacaine hydrochloride

CAS: 18010-40-7 F: C18H29ClN2O W: 324.89

Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.B
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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.