Blockade effects of BIBN4096BS on CGRP-induced inhibition on whole-cell K+ currents in spinal dorsal horn neuron of rats.

Calcitonin gene-related peptide (CGRP) plays an important role in the transmission and modulation of nociceptive information in the spinal cord. BIBN4096BS, a nonpeptide CGRP receptor antagonist, has been shown to be efficiency in clinical migraine treatment. The present study was performed to investigate the effects of BIBN4096BS on the CGRP-induced inhibition to whole-cell K(+) currents in spinal wide dynamic range (WDR) neuron of rats. Application of BIBN4096BS inhibited the neuronal activity of WDR neurons in lumbar dorsal horn of the spinal cord in rats tested by extracellular recording method. Furthermore, CGRP induced inhibition on whole-cell K(+) currents in cultured dorsal horn neurons of rats tested by whole-cell patch-clamp recording, and the effect was significantly blocked by BIBN4096BS. The results indicate that BIBN4096BS may produce antinociceptive effects at the spinal level in rats.