mepivacaine

Mepivacaine (Carbocaine) is an amide compound for local anaesthesia that causes transient loss of self-consciousness in humans or animals. mepivacaine acts by binding to specific voltage-gated sodium channels in nerve cell membranes, inhibiting sodium inward flow and membrane depolarisation. mepivacaine is indicated for nerve blocks and epidurals.

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

Articaine hydrochloride (Hoe-045), a thiophene-containing local anesthetic, is pharmacologically similar to mepivacaine.

Dexivacaine is an type of anesthetic.

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM 40% & 20 μM 60% at pH 9.0, 5 nM 28% & 3 μM 72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM 39% & 10 μM 61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1 2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).