Oz Murat, Tchugunova Yulia, Dinc Meral
NIDA/IRP Cellular Neurobiology Branch, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
Naunyn Schmiedebergs Arch Pharmacol. 2003 Jan;367(1):80-5. doi: 10.1007/s00210-002-0643-x. Epub 2002 Nov 27.
Ethanol has been reported to modulate arterial dilation and insulin secretion. ATP-inhibited K+ channels (K(ATP)) are reported to have regulatory roles during these events. In the present study, the effect of ethanol on K+ currents activated by the K(ATP) channel opener cromakalim was investigated in follicular cells of Xenopus oocytes. The results indicate that ethanol in the concentration range of 10-300 mM (approximately 0.06%-2% v/v) reversibly inhibits the cromakalim-induced K+ currents. The 50% of maximal ethanol effect was obtained at 53 mM. Inhibition of cromakalim-activated K+ current by ethanol was non-competitive. In oocytes treated with the Ca2+-chelator BAPTA, inhibition of cromakalim-induced K+ currents by ethanol was not altered, suggesting that Ca2+-activated second messenger pathways were not involved in the actions of ethanol. Similarly, currents activated by 8-Br-cAMP were also inhibited by ethanol, but the ethanol inhibition of 8-Br-cAMP-activated currents was significantly less than inhibition of cromakalim-activated currents by ethanol. These results indicate that cromakalim-activated K+ currents in follicular cells of Xenopus oocytes were modulated by ethanol.
据报道,乙醇可调节动脉扩张和胰岛素分泌。据报道,ATP抑制性钾通道(K(ATP))在这些过程中具有调节作用。在本研究中,研究了乙醇对非洲爪蟾卵母细胞滤泡细胞中由K(ATP)通道开放剂克罗卡林激活的钾电流的影响。结果表明,浓度范围为10-300 mM(约0.06%-2% v/v)的乙醇可逆地抑制克罗卡林诱导的钾电流。乙醇最大效应的50%在53 mM时获得。乙醇对克罗卡林激活的钾电流的抑制是非竞争性的。在用Ca2+螯合剂BAPTA处理的卵母细胞中,乙醇对克罗卡林诱导的钾电流的抑制没有改变,这表明Ca2+激活的第二信使途径不参与乙醇的作用。同样,由8-溴-cAMP激活的电流也被乙醇抑制,但乙醇对8-溴-cAMP激活电流的抑制明显小于对克罗卡林激活电流的抑制。这些结果表明,非洲爪蟾卵母细胞滤泡细胞中克罗卡林激活的钾电流受乙醇调节。