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.
Hou
Jun-Feng
JF
Laboratory of Neurobiology and National Laboratory of Biomembrane and Membrane Biotechnology, College of Life Sciences, Peking University, Beijing 100871, People's Republic of China.
Yu
Long-Chuan
LC
D000818:Animals; D000831:Animals, Newborn; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D002478:Cells, Cultured; D008161:Lumbosacral Region; D008297:Male; D018408:Patch-Clamp Techniques; D010879:Piperazines / Q000494:pharmacology*; D020671:Posterior Horn Cells / Q000187:drug effects* / Q000502:physiology; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D015221:Potassium Channels / Q000502:physiology*; D011799:Quinazolines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D018015:Receptors, Calcitonin Gene-Related Peptide / Q000502:physiology*
D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D010879:Piperazines; D026902:Potassium Channel Blockers; D015221:Potassium Channels; D011799:Quinazolines; D018015:Receptors, Calcitonin Gene-Related Peptide; C406305:olcegepant