精氨酸加压素对大鼠背根神经节神经元GABA激活电流的增强作用（英文）

发布时间：2018-04-25 02:28

本文选题：精氨酸加压素 + GABA激活电流　；参考：《生理学报》2014年06期

【摘要】：越来越多的研究表明,精氨酸加压素(arginine vasopressin,AVP)在痛觉调制中具有镇痛作用。已报道的研究专注于AVP镇痛的中枢作用机制,而本研究旨在研究AVP镇痛的的外周作用机制。应用全细胞膜片钳技术,在急性分离的大鼠背根神经节(DRG)神经元上,观察AVP对GABA激活电流(IGABA)的增强作用以及AVP对GABAA受体功能的影响。结果显示,AVP(1×10-10~1×10-5 mol/L)预处理后,IGABA增大,GABA剂量效应曲线上移,IGABA的最大值较之对照增加约49.1%;而EC50值几乎不变,表示此种加强为非竞争性的,而且AVP对GABA电流的作用可能是电压非依赖性的。AVP对IGABA的加强作用几乎完全被V1a受体的拮抗剂SR49059(3×10-6 mol/L)阻断。二次钳压技术胞内透析非水解GDP类似物GDP-β-S(5×10-4 mol/L)或PKC抑制剂GF109203X(2×10-6 mol/L)也可以阻断AVP对IGABA的加强作用。以上结果提示,AVP经由G蛋白耦联受体以及PKC信号通路上调DRG神经元GABAA受体的功能,可能是其诱导镇痛作用的基础。
[Abstract]:More and more studies have shown that arginine vasopressin (AVP) plays an analgesic role in pain modulation. The reported studies focus on the central mechanism of AVP analgesia, while this study aims to study the peripheral mechanism of AVP analgesia. The effects of AVP on GABA activated current (IGABA) and the effect of AVP on the function of GABAA receptor were observed in rat dorsal root ganglion (DRG) neurons by whole-cell patch clamp technique. The results showed that the maximum value of EC50 increased by 49.1%, and the EC50 value was almost unchanged, indicating that the enhancement was non-competitive after pretreatment with 1 脳 10 ~ (-10) ~ (10 ~ (-10)) mol 路L ~ (-1) EC50, and the maximum value of IGABA was increased by 49.1% compared with the control. Moreover, the effect of AVP on GABA current may be voltage independent. AVP's enhanced effect on IGABA was almost completely blocked by the V1a receptor antagonist SR49059(3 脳 10-6 mol / L. Secondary clamp technique could also block the enhancement of IGABA by AVP, a non-hydrolyzed GDP analogue GDP- 尾 -Sn 5 脳 10 -4 mol / L) or PKC inhibitor GF109203X(2 脳 10 -6 mol / L. These results suggest that AVP up-regulates the function of DRG neuron GABAA receptor through G protein coupled receptor and PKC signaling pathway, which may be the basis of its analgesic effect.
【作者单位】：生物资源绿色转化湖北省协同创新中心湖北大学生命科学学院;湖北科技学院药学院;
【基金】：supported by the grants from the National Natural Science Foundation of China(No.30500328,31071679,31272050 and 31301675) the Key Scientific Project of Hubei Provincial Education Department,China(No.D20091007) the Natural Science Foundation of Hubei Province,China(No.2010CDB04504)
【分类号】：R363

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