Laboratory of Neurobiology and National Laboratory of Biomembrane and Membrane Biotechnology, College of Life Sciences, Peking University, Beijing 100871, People's Republic of China.
Neurosci Lett. 2010 Jan 18;469(1):15-8. doi: 10.1016/j.neulet.2009.11.035. Epub 2009 Nov 18.
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.
降钙素基因相关肽（CGRP）在脊髓中痛觉信息的传递和调制中起重要作用。BIBN4096BS，一种非肽 CGRP 受体拮抗剂，已被证明在偏头痛的临床治疗中有效。本研究旨在探讨 BIBN4096BS 对 CGRP 诱导的大鼠脊髓宽动态范围（WDR）神经元全细胞 K(+)电流抑制的影响。通过细胞外记录方法检测到 BIBN4096BS 抑制了大鼠脊髓背角 WDR 神经元的神经元活动。此外，通过全细胞膜片钳记录法检测到 CGRP 诱导培养的大鼠背角神经元的全细胞 K(+)电流抑制，BIBN4096BS 可显著阻断该作用。结果表明，BIBN4096BS 可能在大鼠脊髓水平产生镇痛作用。
