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Aroma–oil compounds derived from plants have a variety of clinical effects including local anesthesia. We have previously reported that various aroma–oil compounds reduce the peak amplitudes of fast–conducting and Na+–channel blocker tetrodotoxin–sensitive compound action potentials (CAPs) recorded from the frog sciatic nerve in a manner dependent on their chemical structures. The present study further examined this structure– activity relationship by applying the air–gap method to the frog sciatic nerve. Cyclic alcohols ((+)–borneol, (–)–borneol, α–terpineol), chain alcohols ((–)– linalool, citronellol, geraniol) and esters (bornyl acetate, geranyl acetate) reduced CAP peak amplitudes with the half–maximal inhibitory concentration (IC50) values of 1.5 mM, 2.3 mM, 2.7 mM, 2.0 mM, 0.35 mM, 0.53 mM, 0.44 mM and 0.51 mM, respectively. This IC50 value for (–)–linalool was similar to that for (±)–linalool (1.7 mM), a value as reported previously. On the other hand, hydrocarbon (p–cymene) at a high concentration such as 2 mM reduced CAP amplitude by only 20%. The efficacy sequence of the aroma–oil compounds was esters ≧ alcohols > hydrocarbons, and was thus consistent with one reported previously, i.e., phenols ≧ aldehydes ≧ esters > alcohols > ketones > oxides ≫ hydrocarbons. There was a variation in IC50 value among the alcohols used; chain alcohols were more effective in inhibiting CAPs than cyclic ones. Similar IC50 values of (–)–linalool and (±)– linalool and also of (+)–borneol and (–)–borneol indicate no difference in efficacy between the steroisomers in inhibiting CAPs. There was no correlation between IC50 value for CAP inhibition by aroma–oil compound and its octanol–water partition coefficient value. The present study confirmed that aroma–oil compounds inhibit nerve conduction in a manner specific to their chemical structures.

Inhibition of frog sciatic nerve compound action potentials by aroma-oil compounds in a manner dependent on their chemical structures