A substrate for AChE and an agonist of α4β2-subunit containing nAChRs
Acetylthiocholine is a substrate for acetylcholinesterase (AChE) and an agonist of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs).1,2 It binds to α4β2 subunit-containing nAChRs in SH-EP1 cells (IC50 = 7.1 µM for the human receptor) and induces rubidium efflux in an agonist-induced rubidium efflux assay (EC50 = 100 µM).2 Acetylthiocholine has been used as part of a thiocholine sensor for the detection of pesticides in complex sample types, such as soil, groundwater, and spinach.1
1.Chen, L., Tian, X., Li, Y., et al.Broad-spectrum pesticide screening by multiple cholinesterases and thiocholine sensors assembled high-throughput optical array systemJ. Hazard. Mater.402123830(2021) 2.Eaton, J.B., Peng, J.-H., Schroeder, K.M., et al.Characterization of human α4β2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cellsMol. Pharmacol.64(6)1283-1294(2003)
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