Local anesthetics inhibit glutamatergic transmission in spinal dorsal horn neurons

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It is well established that local anesthetics block impulses in peripheral nerves through the inhibition of voltage-gated sodium channels. The glutamate receptors play an important role in the central nervous system, mediating rapid excitatory neurotransmission. In this study, we showed that local anesthetics inhibited the NMDA-type glutamate receptors in spinal dorsal horn neurons. These findings raise the possibility that the antinociceptive effect of bupivacaine may be due to direct modulation of NMDA receptors in superficial dorsal horn. In addition to voltage-gated sodium channels, the NMDA-type glutamate receptors are also important for anesthesia and analgesia induced by local anesthetics.