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5-羟色胺抑制P2X2受体通道孔突变体。

5-Hydroxytryptamine inhibits P2X2 receptor channel pore mutants.

作者信息

Nakazawa K, Ohno Y

机构信息

Division of Pharmacology, National Institute of Health Sciences, Tokyo, Japan.

出版信息

Cell Mol Neurobiol. 1999 Oct;19(5):665-9. doi: 10.1023/a:1006940720038.

Abstract
  1. 5-Hydroxytryptamine (10 microM) enhanced ionic current mediated through the wild-type P2X2 receptor/channel expressed in Xenopus oocytes. 2. 5-Hydroxytryptamine (10 microM) inhibited a current mediated through P2X2 receptor/channel mutants when Thr330 or Asn333 was replaced with Ile (T330I and N333I). 3. Our results suggest that neutralization of Thr330 or Asn333 exposes a high-affinity, inhibitory binding site for 5-hydroxytryptamine. This implies that 5-hydroxytryptamine interacts with the P2X2 receptor/channel at their channel pores.
摘要
  1. 5-羟色胺(10微摩尔)增强了通过非洲爪蟾卵母细胞中表达的野生型P2X2受体/通道介导的离子电流。2. 当苏氨酸330或天冬酰胺333被异亮氨酸取代(T330I和N333I)时,5-羟色胺(10微摩尔)抑制了通过P2X2受体/通道突变体介导的电流。3. 我们的结果表明,苏氨酸330或天冬酰胺333的中和暴露了一个对5-羟色胺具有高亲和力的抑制性结合位点。这意味着5-羟色胺在其通道孔处与P2X2受体/通道相互作用。

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