Protein kinase C activators decrease dopamine uptake into striatal synaptosomes.
Protein kinase C activators decrease dopamine uptake into striatal synaptosomes.
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发表时间：
1996-06
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通讯作者：
B. J. Copeland;V. Vogelsberg;N. Neff;Maria Hadjiconstantinou
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作者：
B. J. Copeland;V. Vogelsberg;N. Neff;Maria Hadjiconstantinou
蛋白激酶C激活剂phorbol 12-肉豆酸酯13-乙酸酯（PMA）和n-1,2二辛烷甘油（DiC8）均可减少纹状体突触体对多巴胺的摄取，而无活性phorbol酯4 α -PMA则没有影响。PMA和DiC8的洗脱未能逆转摄取的减少。动力学分析表明，转运体的表观V（max）下降，但K(m)没有变化。PMA和DiC8均不影响mazindol与多巴胺转运体的结合。用蛋白激酶抑制剂staurosporine预孵育可阻止dic8诱导的多巴胺摄取减少。此外，蛋白磷酸酶抑制剂冈田酸本身降低了多巴胺的摄取，并增强了dic8诱导的摄取减少。这些发现支持蛋白激酶C在调节多巴胺转运蛋白活性中的作用。
Incubation with either of the protein kinase C activators phorbol 12-myristate 13-acetate (PMA) and sn-1,2 dioctanoylglycerol (DiC8) decreased the uptake of dopamine into striatal synaptosomes, whereas the inactive phorbol ester 4 alpha-PMA had no effect. Washout of PMA and DiC8 failed to reverse the decrease in uptake. Kinetic analysis showed a decrease in the apparent V(max) for the transporter without changes in the K(m). Neither PMA nor DiC8 affected mazindol binding to the dopamine transporter. Preincubation with the protein kinase inhibitor staurosporine prevented the DiC8-induced decrease of dopamine uptake. Furthermore, the protein phosphatase inhibitor okadaic acid decreased dopamine uptake by itself and enhanced the DiC8-induced reduction of uptake. These findings support a role for protein kinase C in modulating dopamine transporter activity.