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首页> 外文期刊>Biochemical Pharmacology >Multiple regulatory actions of 2-guanidine-4-methylquinazoline (GMQ), an agonist of acid-sensing ion channel type 3, on ionic currents in pituitary GH(3) cells and in olfactory sensory (Rolf B1.T) neurons
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Multiple regulatory actions of 2-guanidine-4-methylquinazoline (GMQ), an agonist of acid-sensing ion channel type 3, on ionic currents in pituitary GH(3) cells and in olfactory sensory (Rolf B1.T) neurons

机译：2-胍汀-4-甲基喹唑啉（GMQ），酸感测离子通道3型激动剂的多种调节作用，对垂体GH（3）细胞的离子电流和嗅觉感觉（Rolf B1.T）神经元

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摘要

GMQ (2-guanidine-4-methylquinazoline or N-(4-methyl-2-quinazolinyl)-guanidine hydrochloride), an agonist of acid-sensing ion channel type 3, has been increasingly used for in vivo studies of alternations in nociceptic behavior. In this study, we tried to investigate whether GMQ has any possible effect on other types of ion channels. Addition of GMQ to pituitary GH3 cells raised the amplitude of Ca2+-activated K+ currents (I-k(Ca)), which was reversed by verruculogen or PF1022A, but not by TRAM-39. Under inside-out current recordings, addition of GMQ into bath enhanced the probability of large-conductance Ca2+-activated K+ (BKCa) channels with an EC50 value of 0.95 mu M. The activation curve of BKCa channels during exposure to GMQ shifted to a lower depolarized potential, with no change in the gating charge of the curve; however, there was a reduction of free energy for channel activation in its presence. As cells were exposed to GMQ, the amplitude of ion currents were suppressed, including delayed rectifying K+ current, voltage-gated Na+ and L-type Ca2+ currents. In Rolf B1.T olfactory sensory neuron, addition of GMQ was able to induce inward current and to suppress peak I-Na. Taken together, findings from these results indicated that in addition to the activation of ASIC3 channels, this compound might directly produce additional actions on various types of ion channels. Caution should be taken in the interpretation of in vivo experimental results when GMQ or other structurally similar compounds are used as targets to characterize the potential functions of ASIC3 channels.
机译：GMQ（2-胍 - 4-甲基喹唑啉或N-（4-甲基-2-喹唑啉基） - 盐酸盐型激动剂，酸感测离子通道3型的激动剂，越来越多地用于伤害行为中的替代的体内研究。在这项研究中，我们试图调查GMQ是否对其他类型的离子通道产生了任何影响。添加GMQ至垂体GH3细胞提高了Ca2 +活化的k +电流的幅度（I-k（Ca）），其被疣素或PF1022a反转，但不是由电车轨道-39逆转。在内外电流记录下，将GMQ添加到浴中，增强了大导电CA2 + -Activated k +（BKCA）通道的概率，EC50值为0.95 mu m。在接触GMQ期间BKCA通道的激活曲线移位到较低去极化的电位，曲线的门控电荷没有变化;然而，在存在的情况下，减少了可自由能量的通道激活。随着细胞暴露于GMQ，抑制了离子电流的幅度，包括延迟整流K +电流，电压门控Na +和L型Ca2 +电流。在Rolf B1.T嗅觉中神经元中，添加GMQ能够诱导内向电流并抑制峰I-NA。从这些结果中占据，结果表明，除了ASIC3通道的激活外，该化合物还可以直接在各种类型的离子通道上产生额外的作用。小心应采取在体内实验结果的解释中，当使用GMQ或其他结构类似的化合物用作表征ASIC3通道的潜在功能的靶标时。

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