β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC50=76 μM) and cholinesterase (ChE; IC50=40 μM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC50=1 mM)[1][2].
At ChA-inhibiting concentrations, β-NETA had no effect on muscarinic receptors, ganglion nicotinic receptors, skeletal muscle nicotinic receptors, cholinesterase, or carnitine acetyltransferase. At concentrations above the ChA-inhibiting IC50 value, β-NETA antagonized acetylcholine (ED50 = 100 μM), histamine, and KCl-induced guinea pig ileal longitudinal muscle contraction [2].
References:
[1]. Sastry BV, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.
[2]. B V Sastry, et al. 2-(alpha-Naphthoyl)ethyltrimethylammonium iodide and its beta-isomer: new selective, stable and fluorescent inhibitors of choline acetyltransferase. J Pharmacol Exp Ther. 1988 Apr;245(1):72-80.
β-NETA 是一种有效的，非竞争性的胆碱乙酰转移酶 (ChA；IC50=76 μM) 和胆碱酯酶 (ChE; IC50=40 μM) 抑制剂。β-NETA 微弱的抑制乙酰胆碱酯 (AChE; IC50=1 mM)。
在抑制 ChA 的浓度下，β-NETA 对毒蕈碱受体、神经节烟碱受体、骨骼肌烟碱受体、胆碱酯酶或肉碱乙酰转移酶没有影响。在高于抑制 ChA 的 IC50 值的浓度下，β-NETA 拮抗乙酰胆碱 (ED50=100 μM)、组胺和 KCl 诱导的豚鼠回肠纵肌收缩的作用。