Feuerstein T J, Allgaier C, Hertting G
Institut für Pharmakologie und Toxikologie, Universität Freiburg, F.R.G.
Eur J Pharmacol. 1987 Jul 23;139(3):267-72. doi: 10.1016/0014-2999(87)90583-8.
Protein kinase C (PKC)-activating phorbol esters enhanced the electrically evoked 5-HT release from rabbit hippocampal slices preincubated with [3H]5-HT. The release was diminished by polymyxin B, an inhibitor of PKC. These results are compatible with a stimulatory effect of PKC on the 5-HT release induced by action potentials. The mutual effects of PKC affecting drugs on 5-HT release suggest a functional but not a competitive interaction. The attenuation or the enhancement of effects of 5-HT autoreceptor ligands at various 5-HT biophase concentrations found after PKC-affecting drugs are in line with the view that autoreceptor-mediated events are not directly influenced by the enzyme PKC.
蛋白激酶C(PKC)激活剂佛波酯增强了预先用[3H]5-羟色胺(5-HT)孵育的兔海马切片中电诱发的5-HT释放。该释放被PKC抑制剂多粘菌素B所减弱。这些结果与PKC对动作电位诱导的5-HT释放的刺激作用相一致。PKC作用药物对5-HT释放的相互影响表明是功能性而非竞争性相互作用。在PKC作用药物处理后,在不同5-HT生物相浓度下发现5-HT自身受体配体效应的减弱或增强,这与自身受体介导的事件不受PKC酶直接影响的观点相符。