Schoffelmeer A N, Wardeh G, Mulder A H
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jul;330(1):74-6. doi: 10.1007/BF00586712.
The adenylate cyclase activator forskolin as well as 8-bromo-cyclic AMP enhanced the electrically evoked release of 3H-noradrenaline and 3H-5-hydroxytryptamine from superfused rat neocortical slices and that of 3H-dopamine from neostriatal slices with comparable EC50's of about 0.5 and 50 microM, respectively, without affecting spontaneous tritium efflux. The phosphodiesterase inhibitor ZK 62771 (3-100 microM) also enhanced 3H-noradrenaline and 3H-dopamine release but slightly reduced 3H-5-hydroxytryptamine release. However, this drug profoundly enhanced spontaneous tritium release in the latter case. The facilitatory effect of forskolin (0.3 microM) on the release of the amine neurotransmitters was potentiated in the presence of ZK 62771 (30 microM). Therefore, cyclic AMP appears to exert a general facilitatory effect on the release of these biogenic amines from central nerve terminals.
腺苷酸环化酶激活剂福斯高林以及8-溴环磷酸腺苷增强了从灌流大鼠新皮质切片中电诱发的3H-去甲肾上腺素和3H-5-羟色胺的释放,以及从新纹状体切片中电诱发的3H-多巴胺的释放,其半数有效浓度(EC50)分别约为0.5和50微摩尔,且不影响自发的氚外流。磷酸二酯酶抑制剂ZK 62771(3 - 100微摩尔)也增强了3H-去甲肾上腺素和3H-多巴胺的释放,但略微降低了3H-5-羟色胺的释放。然而,在后者的情况下,这种药物显著增强了自发的氚释放。在存在ZK 62771(30微摩尔)的情况下,福斯高林(0.3微摩尔)对胺类神经递质释放的促进作用增强。因此,环磷酸腺苷似乎对这些生物胺从中枢神经末梢的释放发挥普遍的促进作用。