Lüscher C, Jan L Y, Stoffel M, Malenka R C, Nicoll R A
Department of Cellular and Molecular Pharmacology, University of California, San Francisco 94143, USA.
Neuron. 1997 Sep;19(3):687-95. doi: 10.1016/s0896-6273(00)80381-5.
To study the role of G protein-coupled, inwardly rectifying K+ (GIRK) channels in mediating neurotransmitter actions in hippocampal neurons, we have examined slices from transgenic mice lacking the GIRK2 gene. The outward currents evoked by agonists for GABA(B) receptors, 5HT1A receptors, and adenosine A1 receptors were essentially absent in mutant mice, while the inward current evoked by muscarinic receptor activation was unaltered. In contrast, the presynaptic inhibitory action of a number of presynaptic receptors on excitatory and inhibitory terminals was unaltered in mutant mice. These included GABA(B), adenosine, muscarinic, metabotropic glutamate, and NPY receptors on excitatory synapses and GABA(B) and opioid receptors on inhibitory synapses. These findings suggest that a number of G protein-coupled receptors activate the same class of postsynaptic K+ channel, which contains GIRK2. In addition, the GIRK2 channels play no role in the inhibition mediated by presynaptic G protein-coupled receptors, suggesting that the same receptor can couple to different effector systems according to its subcellular location in the neuron.
为了研究G蛋白偶联内向整流钾离子(GIRK)通道在介导海马神经元神经递质作用中的作用,我们检测了缺乏GIRK2基因的转基因小鼠的脑片。在突变小鼠中,GABA(B)受体、5HT1A受体和腺苷A1受体激动剂诱发的外向电流基本缺失,而毒蕈碱受体激活诱发的内向电流未改变。相比之下,突变小鼠中一些突触前受体对兴奋性和抑制性终末的突触前抑制作用未改变。这些受体包括兴奋性突触上的GABA(B)、腺苷、毒蕈碱、代谢型谷氨酸和神经肽Y受体,以及抑制性突触上的GABA(B)和阿片受体。这些发现表明,许多G蛋白偶联受体激活了同一类包含GIRK2的突触后钾离子通道。此外,GIRK2通道在突触前G蛋白偶联受体介导的抑制中不起作用,这表明同一受体可根据其在神经元中的亚细胞定位与不同的效应系统偶联。