Holz G G, Dunlap K, Kream R M
Department of Physiology, Tufts University School of Medicine, Boston, Massachusetts 02111.
J Neurosci. 1988 Feb;8(2):463-71. doi: 10.1523/JNEUROSCI.08-02-00463.1988.
The mechanism by which dihydropyridines (DHPs) modulate the electrically evoked or KCI-induced release of substance P (SP) from embryonic chick dorsal root ganglion (DRG) neurons was investigated in the present study. The release of SP, as measured by radioimmunoassay (RIA), was characterized in terms of its dependence on extracellular calcium ion, its stimulus-response relationship, its sensitivity to the calcium-channel blocker omega conus toxin (omega-CgTx), and its modulation by the DHPs Bay K 8644 and nifedipine. Here it is reported that omega-CgTx (1 microM) blocked the electrically evoked release of SP. In contrast, the calcium-channel agonist Bay K 8644 (5 microM) facilitated the release of SP (by 45%), whereas the calcium-channel antagonist nifedipine (5 microM) was without effect. When the release of SP was triggered by depolarization of cultures with 60 mM KCI, the actions of the DHPs became much more pronounced. Under these conditions, Bay K 8644 facilitated (by 115%), whereas nifedipine inhibited (by 58%), peptide secretion. Voltage-clamp analysis of DRG cell calcium currents demonstrated that these actions of omega-CgTx, Bay K 8644, and nifedipine are explicable in terms of their effects on the slowly inactivating (L-type) calcium current. On the basis of these findings, it is suggested that the SP release mechanism exhibits DHP sensitivity due to the involvement of L-type calcium channels in the neurosecretory process. This model predicts that the voltage and time-dependent antagonist actions of nifedipine are sufficient to explain its failure to inhibit the electrically evoked release of SP.
在本研究中,对二氢吡啶类(DHPs)调节胚胎鸡背根神经节(DRG)神经元中电诱发或氯化钾诱导的P物质(SP)释放的机制进行了研究。通过放射免疫分析(RIA)测定的SP释放,根据其对细胞外钙离子的依赖性、刺激-反应关系、对钙通道阻滞剂ω-芋螺毒素(ω-CgTx)的敏感性以及DHPs Bay K 8644和硝苯地平对其的调节作用进行了表征。在此报告,ω-CgTx(1微摩尔)阻断了电诱发的SP释放。相反,钙通道激动剂Bay K 8644(5微摩尔)促进了SP的释放(增加了45%),而钙通道拮抗剂硝苯地平(5微摩尔)则无作用。当用60毫摩尔氯化钾使培养物去极化触发SP释放时,DHPs的作用变得更加明显。在这些条件下,Bay K 8644促进了(增加了115%),而硝苯地平抑制了(减少了58%)肽分泌。DRG细胞钙电流的电压钳分析表明,ω-CgTx、Bay K 8644和硝苯地平的这些作用可以根据它们对缓慢失活(L型)钙电流的影响来解释。基于这些发现,提示SP释放机制表现出对DHPs敏感,这是由于L型钙通道参与了神经分泌过程。该模型预测,硝苯地平的电压和时间依赖性拮抗作用足以解释其未能抑制电诱发的SP释放。