Purinergic P2X2 receptor desensitization depends on coupling between ectodomain and C-terminal domain
Purinergic P2X2 receptor desensitization depends on coupling between ectodomain and C-terminal domain
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DOI：
10.1124/mol.62.5.1187
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发表时间：
2002-11-01
影响因子：
3.6
通讯作者：
Stojilkovic, SS
中科院分区：
文献类型：
--
作者：
He, ML;Koshimizu, TA;Stojilkovic, SS
野生型P2X(2)嘌呤能受体(P2X(2a)R)及其缺失细胞内Val(370)-Gln(438)C末端序列的剪接形式(P2X(2b)R)对ATP刺激的反应具有相似的EC50值和峰值电流/钙反应，但以受体特异性的方式减敏。P2X(2a)R减敏较慢，而P2X(2b)R减敏较快。我们研究了不同激动剂和取代胞外结构域对P2X(2a)R和P2X(2b)R钙信号模式的影响。这两种受体对激动剂的EC50值(根据峰值钙反应估计)和IC50值(根据钙信号脱敏速度估计)相似，顺序为2-MES-ATP小于或等于ATP小于或等于ATPGammaS<；BzATP
The wild-type P2X(2) purinergic receptor (P2X(2a)R) and its splice form lacking the intracellular Val(370)-Gln(438) C-terminal sequence (P2X(2b)R) respond to ATP stimulation with comparable EC50 values and peak current/calcium responses but desensitize in a receptor-specific manner. P2X(2a)R desensitizes slowly and P2X(2b)R desensitizes rapidly. We studied the effects of different agonists, and of substituting the ectodomain, on the pattern of calcium signaling by P2X(2a)R and P2X(2b)R. Both receptors showed similar EC50 values (estimated from the peak calcium response) and IC50 values (estimated from the rate of calcium signal desensitization) for agonists, in the order 2-MeS-ATP less than or equal to ATP less than or equal to ATPgammaS < BzATP