Ikeuchi Y, Nishizaki T
Department of Physiology, Kobe University School of Medicine, Japan.
Biochem Biophys Res Commun. 1996 Jan 5;218(1):67-71. doi: 10.1006/bbrc.1996.0013.
P2 purinoceptor agonists produced whole-cell potassium currents in cerebellar neurons with the order of potency 2-methylthio ATP (2-MeSATP) > ADP > ATP > adenosine > alpha,beta- methylene ATP > AMP > UTP. In the outside-out patch clamp configuration, 2-MeSATP evoked single channel currents with two major classes of slope conductances without latency. The currents were blocked by a G-protein inhibitor, GDP beta S, although they were not affected by a phospholipase C inhibitor, a selective protein kinase C or A inhibitor. In contrast, a potent G-protein activator, GTP gamma S, produced single channel currents with same conductances as those of the currents induced by 2-MeSATP. These provide an indication that the P2 purinoceptor-operated potassium channel is regulated by the beta gamma subunits of a G-protein.
P2嘌呤受体激动剂在小脑神经元中产生全细胞钾电流,其效力顺序为2-甲硫基ATP(2-MeSATP)>ADP>ATP>腺苷>α,β-亚甲基ATP>AMP>UTP。在外侧膜片钳配置中,2-MeSATP诱发单通道电流,有两类主要的斜率电导且无潜伏期。这些电流被G蛋白抑制剂GDPβS阻断,尽管它们不受磷脂酶C抑制剂、选择性蛋白激酶C或A抑制剂的影响。相反,一种有效的G蛋白激活剂GTPγS产生的单通道电流与2-MeSATP诱导的电流具有相同的电导。这些表明P2嘌呤受体操纵的钾通道受G蛋白的βγ亚基调节。