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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（SLC22A4）介导的乙酰胆碱转运的生理阳离子调节。对非神经胆碱能系统的影响。

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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：本研究旨在探讨生理离子对重组人有机阳离子转运蛋白新型1（hOCTN1）催化的乙酰胆碱转运的影响，从而参与了非神经元胆碱能系统的功能。蛋白脂质体的实验模型重建已经使用了通过在大肠杆菌中过表达获得的hOCTN1转运蛋白的载体。在存在不同阳离子的情况下，遵循[（3）H]乙酰胆碱在蛋白脂质体系统中的吸收和流出，模拟细胞环境。内部K（+）受到刺激，而外部Na（+）强烈抑制[（（ 3）H]乙酰胆碱在脂质体中。外部K（+）也产生强抑制作用，而Mg（2+）或蔗糖则没有作用。不同的是，[（3）H]乙酰胆碱从蛋白脂质体的流出不受外部或内部Na（+）的影响，而仅受内部K（+）的刺激。通过剂量响应分析的Na（+）抑制，得出1.3 mM的IC（50）。 Na（+）效应的动力学分析显示竞争性抑制乙酰胆碱摄取的类型，即Na（+）与乙酰胆碱的相同外部结合位点相互作用，Ki为1.2mM。hOCTN1催化的乙酰胆碱转运显示不对称Na（+）调节。由于脂质体膜中转运蛋白的取向与天然膜中的转运蛋白的取向相同，并且基于抑制的侧面，生理性乙酰胆碱主要由转运蛋白输出。这暗示着在非神经元组织中的自分泌和旁分泌作用中起作用。

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