Scholze Thomas, Moskvina Eugenia, Mayer Martina, Just Herwig, Kubista Helmut, Boehm Stefan
Department of Pharmacology, University of Vienna, A-1090 Vienna, Austria.
J Neurosci. 2002 Jul 15;22(14):5823-32. doi: 10.1523/JNEUROSCI.22-14-05823.2002.
Bradykinin has long been known to excite sympathetic neurons via B(2) receptors, and this action is believed to be mediated by an inhibition of M-currents via phospholipase C and inositol trisphosphate-dependent increases in intracellular Ca(2+). In primary cultures of rat superior cervical ganglion neurons, bradykinin caused an accumulation of inositol trisphosphate, an inhibition of M-currents, and a stimulation of action potential-mediated transmitter release. Blockade of inositol trisphosphate-dependent signaling cascades failed to affect the bradykinin-induced release of noradrenaline, but prevented the peptide-induced inhibition of M-currents. In contrast, inhibition or downregulation of protein kinase C reduced the stimulation of transmitter release, but not the inhibition of M-currents, by bradykinin. In cultures of superior cervical ganglia, classical (alpha, betaI, betaII), novel (delta, epsilon), and atypical (zeta) protein kinase C isozymes were detected by immunoblotting. Bradykinin induced a translocation of Ca(2+)-independent protein kinase C isoforms (delta and epsilon) from the cytosol to the membrane of the neurons, but left the cellular distribution of other isoforms unchanged. This activation of Ca(2+)-independent protein kinase C enzymes was prevented by a phospholipase C inhibitor. The bradykinin-dependent stimulation of noradrenaline release was reduced by inhibitors of classical and novel protein kinase C isozymes, but not by an inhibitor selective for Ca(2+)-dependent isoforms. These results demonstrate that bradykinin B(2) receptors are linked to phospholipase C to simultaneously activate two signaling pathways: one mediates an inositol trisphosphate- and Ca(2+)-dependent inhibition of M-currents, the other one leads to an excitation of sympathetic neurons independently of changes in M-currents through an activation of Ca(2+)-insensitive protein kinase C.
长期以来,人们已知缓激肽通过B(2)受体兴奋交感神经元,据信该作用是通过磷脂酶C抑制M电流以及肌醇三磷酸依赖性细胞内Ca(2+)增加来介导的。在大鼠颈上神经节神经元的原代培养中,缓激肽导致肌醇三磷酸积累、M电流抑制以及动作电位介导的递质释放刺激。阻断肌醇三磷酸依赖性信号级联反应未能影响缓激肽诱导的去甲肾上腺素释放,但可防止该肽诱导的M电流抑制。相反,蛋白激酶C的抑制或下调减少了缓激肽对递质释放的刺激,但未减少对M电流的抑制。在颈上神经节培养物中,通过免疫印迹检测到经典(α、βI、βII)、新型(δ、ε)和非典型(ζ)蛋白激酶C同工酶。缓激肽诱导Ca(2+)非依赖性蛋白激酶C同工型(δ和ε)从神经元胞质溶胶转位至细胞膜,但其他同工型的细胞分布未改变。磷脂酶C抑制剂可阻止这种Ca(2+)非依赖性蛋白激酶C酶的激活。经典和新型蛋白激酶C同工酶抑制剂可减少缓激肽依赖性去甲肾上腺素释放刺激,但对Ca(2+)依赖性同工型选择性抑制剂无此作用。这些结果表明,缓激肽B(2)受体与磷脂酶C相连,同时激活两条信号通路:一条介导肌醇三磷酸和Ca(2+)依赖性M电流抑制,另一条通过激活Ca(2+)不敏感蛋白激酶C导致交感神经元兴奋,而与M电流变化无关。