Department of Obstetrics and Gynecology, Higashihiroshima Medical Center, Higashihiroshima, Japan.
Reprod Sci. 2012 Dec;19(12):1285-91. doi: 10.1177/1933719112450333. Epub 2012 Jul 18.
The functional significance of purinergic P2 receptors in the myometrium is unclear. We previously reported the ATP-induced ionic currents in rat myometrial cells, causing uterine contractility. The aim of this study is to determine the main P2X receptors that carry the adenosine triphosphate (ATP)-induced currents.
We cloned predominantly expressed P2X7 receptors from rat myometrium and transfected into cultured COS-7 cells. Reconstructed P2X7 receptor currents were characterized using the whole-cell patch clamp method.
Extracellular ATP induced currents through P2X7 receptors with effective concentration (EC(50)) of 155 μmol/L, without desensitization. The myometrial P2X7 receptor was permeable to multiple monovalent cations with conductances ranked as K(+)>Cs(+)>Li(+)>Na(+). It was activated by P2X receptor agonists, with effectiveness ranked as 2',3'-O-(4-benzoylbenzoyl)-ATP (Bz-ATP)>>ATP>αβ-methylene ATP (αβ-MeATP)>2-methylthio ATP (2-MeSATP)>uridine triphosphate (UTP)>guanosine triphosphate (GTP)>adenosine diphosphate (ADP). These currents were blocked by selective P2X7 receptor antagonists and extracellular Mg(2+).
P2X7 receptors carry ATP-induced currents in rat myometrial cells.
嘌呤能 P2 受体在子宫肌层中的功能意义尚不清楚。我们之前报道了在大鼠子宫肌细胞中,ATP 诱导的离子电流可引起子宫收缩。本研究旨在确定主要的 P2X 受体,这些受体携带三磷酸腺苷 (ATP) 诱导的电流。
我们从大鼠子宫肌层中克隆了主要表达的 P2X7 受体,并转染到培养的 COS-7 细胞中。使用全细胞膜片钳方法对重建的 P2X7 受体电流进行了特征描述。
细胞外 ATP 通过 P2X7 受体诱导电流,其有效浓度 (EC50) 为 155μmol/L,无脱敏现象。子宫 P2X7 受体对多种单价阳离子具有通透性,其电导大小依次为 K(+)>Cs(+)>Li(+)>Na(+)。它被 P2X 受体激动剂激活,效力大小依次为 2',3'-O-(4-苯甲酰基苯甲酰基)-ATP (Bz-ATP)>>ATP>αβ-亚甲基 ATP (αβ-MeATP)>2-甲硫基 ATP (2-MeSATP)>尿苷三磷酸 (UTP)>鸟苷三磷酸 (GTP)>腺苷二磷酸 (ADP)。这些电流被选择性 P2X7 受体拮抗剂和细胞外 Mg2+ 阻断。
P2X7 受体在大鼠子宫肌细胞中携带 ATP 诱导的电流。