Obergrussberger Alison, Haarmann Claudia, Rinke Ilka, Becker Nadine, Guinot David, Brueggemann Andrea, Stoelzle-Feix Sonja, George Michael, Fertig Niels
Nanion Technologies, Munich, Germany.
Curr Protoc Pharmacol. 2014 Jun 16;65:11.13.1-48. doi: 10.1002/0471141755.ph1113s65.
Automated patch clamp devices are now commonly used for studying ion channels. A useful modification of this approach is the replacement of the glass pipet with a thin planar glass layer with a small hole in the middle. Planar patch clamp devices, such as the three described in this unit, are overtaking glass pipets in popularity because they increase throughput, are easier to use, provide for the acquisition of high-quality and information-rich data, and allow for rapid perfusion and temperature control. Covered in this unit are two challenging targets in drug discovery: voltage-gated sodium subtype 1.7 (Na(V)1.7) and nicotinic acetylcholine α7 receptors (nAChα7R). Provided herein are protocols for recording activation and inactivation kinetics of Na(V)1.7, and activation and allosteric modulation of nAChα7R.
自动膜片钳设备如今常用于研究离子通道。这种方法的一种有用改进是用中间有小孔的薄平面玻璃层取代玻璃吸管。平面膜片钳设备,如本单元所述的三种,正越来越受欢迎,因为它们提高了通量,更易于使用,能获取高质量且信息丰富的数据,并允许快速灌注和温度控制。本单元涵盖了药物研发中的两个具有挑战性的靶点:电压门控钠通道亚型1.7(Na(V)1.7)和烟碱型乙酰胆碱α7受体(nAChα7R)。本文提供了记录Na(V)1.7激活和失活动力学以及nAChα7R激活和变构调节的方案。