P2X3在慢性咳嗽中的作用
2021-09-14548P2X受体是由细胞外ATP激活的三聚体配体门控离子通道。当被激活时,小的一价阳离子通过孔。P2X通道已被证明在炎症、内脏和神经病理性疼痛状态中起作用,此外,在气道高反应性、偏头痛、瘙痒和癌痛中也起作用。Z近,P2X2/3和P2X3受体拮抗剂MK-7264(gefapixant)已进入难治性和原因不明的慢性咳嗽的III期临床试验。
Key Publications:
Ford, A.P. & Undem, B.J. 2013. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Frontiers in Cellular Neuroscience
Ford, A.P. 2012. In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signalling
Measuring P2X3 Channels
P2X3 Channels can be measured using automated patch clamp when expressed in cell lines, or using the Orbit instruments when they are recombinantly expressed in bilayers.
High throughput automated patch clamp
Parallel bilayer recordings
Cytotoxicity measurements
Application Notes:
P2X3 - "Activation and inhibition of P2X3 channels recorded on the Patchliner"
Publications using Instruments from Nanion
2019 - Action of MK‐7264 (Gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation
2011 - State-of-the-art automated patch clamp devices: heat activation, action potentials, and high throughput in ion channel screening