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. 2020 Apr 5;13(4):62. doi: 10.3390/ph13040062

Table 6.

Comparison of IC50 values in inhibiting frog or rat sciatic nerve fast-conducting CAPs and TTX-sensitive or -resistant Na+ channels among local anesthetics.

Local Anesthetics Frog
CAP
IC50 (mM)
Rat
CAP
IC50 (mM)
TTX-Sensitive
Na+ Channel
Current
IC50 (mM)
TTX-Resistant
Na+ Channel
Current
IC50 (mM)
References
Amide Type
Lidocaine 0.74 0.28 0.204 0.073 [19,71,148,236]
Ropivacaine 0.34 0.28 [19,236]
Prilocaine 1.8 [26]
Levobupivacaine 0.23 0.264 [23,239]
Bupivacaine 76% reduction
(0.5 mM)
0.027 [23,71]
0.178 [155]
0.190 [204]
Ester Type
Cocaine 0.80 40% reduction
(0.375 mM)
ca. 70% reduction
(0.05 mM)
[20,72,244]
Procaine 2.2 ca. 1 mM 0.060 [27,71,248]
Benzocaine 0.80 37% reduction
(1.3 mM)
[25,59]
Tetracaine 0.014 0.0007 [22,71]
Other Type
Pramoxine 0.21 [26]

Here, when IC50 values are not available, it is partly shown for comparison how CAP and channel current amplitudes are reduced by drugs, where % value indicates the extent of the reduction at the concentration shown in parentheses.