煙堿型乙酰膽堿受體(nAChRs)是一種配體門控離子通道受體,存在于中樞和周圍神經系統的神經元上以及神經肌肉接頭內的肌肉細胞上。nAChRs進一步分為肌肉型(N1)和神經元型(N2)兩種類型,其中肌肉煙堿受體功能是引發骨骼肌中的隨意肌肉運動。在與Ach結合后,煙堿受體特異性誘導效應細胞的細胞膜上形成離子通道,帶正電的離子(陽離子)可以通過該離子通道進入細胞內。離子的流入導致細胞膜去極化并產生動作電位,例如觀察到的肌肉收縮。所以,肌肉型煙堿受體是眾所周知的肌肉松弛劑藥物的靶點。
愛思益普電生理團隊構建了包括α1β1δε nAChR在內的多種煙堿型乙酰膽堿離子通道細胞系以及不同通量的膜片鉗檢測方法,具有豐富的藥物篩選經驗。自動膜片鉗(APC)方便試驗人員獨立操作,并且檢測通量高,我們使用SophionQPatch 48X可以自動化滿足絕大多數離子通道的電生理檢測。
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nAChRα1β1εδ數據展示-自動膜片鉗
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Figure 1. Acetylcholine is the endogenous agonist at muscarinic and nicotinic cholinergic receptors. (a) Dose-response curve ofacetylcholineon α1β1δε nAChR in Qpatch platform. (b)Representative nAChR current agonizedby multiple concentrations of acetylcholinein CHO cells expressing human α1β1δε.
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Figure 2. Adiphenine is an acetylcholine receptor inhibitor used as an antispasmodic drug due to its strong smooth muscle relaxant action.(a) Dose-response curve ofadiphenineinhibition of 8 μM Ach induced α1β1δε nAChRcurrent in Qpatch platform.(b)Representative α1β1δε nAChR current traces induced by 8 µM AChbefore and after application with multiple concentrations ofadiphenine.
