Kuleshov V I, Kozlov N S, Libman N M, Kosmacheva I M, Zhikhareva O D
Biokhimiia. 1981 Oct;46(10):1764-7.
"In vitro" studies have demonstrated that methyl-p-toluene sulfonates of 1-methyl-(ethyl)-3-aryl-benzo(f)quinolinium are highly efficient inhibitors of cholinesterases, the inhibition constants (Ki) for acetylcholinesterase and butyrylcholinesterase being equal to 2.20 +/- 0.49 and 9.43 +/- 0.39 mkM, respectively. The effect of these inhibitors on the enzyme is of competitive - non-competitive type. A certain role in benzo(f)quinoline binding to acetylcholinesterase apparently belongs to the interaction of substituents in the phenyl nucleus with the anionic sites located outside the active surface of the enzyme.
“体外”研究表明，1-甲基-（乙基）-3-芳基-苯并（f）喹啉鎓的对甲苯磺酸甲酯是高效的胆碱酯酶抑制剂，乙酰胆碱酯酶和丁酰胆碱酯酶的抑制常数（Ki）分别等于2.20±0.49和9.43±0.39μM。这些抑制剂对酶的作用属于竞争性-非竞争性类型。苯并（f）喹啉与乙酰胆碱酯酶结合中，苯环上取代基与位于酶活性表面外的阴离子位点之间的相互作用显然起了一定作用。
