A STUDY ON THE BINDIND MODE OF LOCAL ANESTHETICS WITH PHOSPHOLIPID BILAYER AND SODIUM CHANNEL.

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The site of local anesthetics action is well known to be sodium channel. However, several questions have been raised in response to Hille's theory that specific receptor exist for local anesthetics. Local anesthetics can inhibit the passage of the sodium ion by binding to the biomembrane that surrouds the sodium channel, thereby altering the comformation of channel proteins and expressing their pharmacological effect. In this study, NMR was utilized to measure the binding ability of local anesthetics with the phospholipid membrane in order to compare the pharmacological characteristics (potency and toxity) of the anesthetics. The results of the study demonstrate that chemical shift values and the broadening of the choline methyl signal of phospholipid membrane are closely related and that the change of choline methyl signal in the membrane is useful indicator of proximity between the membrane and anesthetics. The results of the study also indicate that the binding ability of local anesthetics toward the phospholipid membrane was found to be directly proportional to the anesthetics potency, suggesting that the biomembrane plays an important role in the action mechanism of local anesthetics.