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首页> 外文期刊>Life sciences >Regulation by physiological cations of acetylcholine transport mediated by human OCTN1 (SLC22A4). Implications in the non-neuronal cholinergic system.
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Regulation by physiological cations of acetylcholine transport mediated by human OCTN1 (SLC22A4). Implications in the non-neuronal cholinergic system.

机译：由人OctN1介导的乙酰胆碱转运的生理阳离子（SLC22A4）调节。 非神经元胆碱能系统的影响。

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This study aimed to investigate the influence of physiological ions on the transport of acetylcholine which is catalyzed by the recombinant human Organic Cation Transporter Novel 1 (hOCTN1), thus being involved in the function of the non neuronal cholinergic system.The experimental model of proteoliposomes reconstituted with the hOCTN1 transporter obtained by over-expression in E. coli has been used. Uptake and efflux of [(3)H]acetylcholine in the proteoliposome system have been followed in the presence of different cations, mimicking the cell environment.Internal K(+) stimulated, while external Na(+) strongly inhibited the uptake of [(3)H]acetylcholine in proteoliposomes. Strong inhibition was exerted also by external K(+) while Mg(2+) or sucrose had no effect. Differently, the efflux of [(3)H]acetylcholine from proteoliposomes was not influenced by external or internal Na(+) and was only marginally stimulated by internal K(+). By dose response analysis of the Na(+) inhibition, an IC(50) of 1.3 mM was derived. The kinetic analysis of the Na(+) effect revealed a competitive type of inhibition on acetylcholine uptake, i.e., Na(+) interacts with the same external binding site of acetylcholine with a Ki of 1.2 mM.Acetylcholine transport catalyzed by hOCTN1 revealed an asymmetric regulation by Na(+). Since the orientation of the transporter in the liposomal membrane is the same as in native membranes, and on the basis of sidedness of inhibition, physiological acetylcholine is principally exported by the transporter. This implies a role in autocrine and paracrine effects in non neuronal tissues.
机译：本研究旨在研究生理离子对由重组人有机阳离子转运蛋白11（HOCTN1）催化的乙酰胆碱转运的影响，从而参与非神经元胆碱能系统的功能。重组蛋白质素体的实验模型使用通过在大肠杆菌中的过表达获得的HOCTN1转运物。在不同阳离子的存在下，在不同阳离子存在下进行了[（3）H]乙酰胆碱的摄取和流出，模仿细胞环境。刺激内部K（+），而外部Na（+）强烈抑制[（ 3）H]乙酰胆碱在蛋白环体中。外部K（+）也施加强烈的抑制，而Mg（2+）或蔗糖无效。不同地，来自蛋白质素体的[（3）H]乙酰胆碱的流出不受外部或内部Na（+）的影响，仅通过内部K（+）略微刺激。通过对Na（+）抑制的剂量反应分析，衍生13mm的IC（50）。 Na（+）效应的动力学分析揭示了乙酰胆碱摄取的竞争类型的抑制作用，即Na（+）与乙酰胆碱的相同外部结合位点相互作用，致核桃催化的乙酰胆碱转运的Ki为催化。揭示不对称Na（+）的调节。由于脂质体膜中的转运物的取向与天然膜中的相同，并且在抑制的等程度的基础上，生理乙酰胆碱主要由转运蛋白出口。这意味着在非神经元组织中的自分泌和旁静脉作用中的作用。

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