Figure 4.
Enzyme inhibition kinetic analysis of duloxetine against human acetylcholinesterase. (A) Nonlinear regression analyses estimated an inhibition constant (Ki) of 65.5 μM for duloxetine against human AChE. Duloxetine behaved as a mixed-competitive inhibitor of AChE. Similar analyses on (B) citalopram and (C) its S-enantiomer, escitalopram, estimated Ki values of 58.9 and 32.8 μM, respectively. The analyses in addition indicated that citalopram behaves like a noncompetitive inhibitor, while escitalopram is a mixed-competitive inhibitor like duloxetine. Thus, escitalopram appears twice as potent an AChE inhibitor as duloxetine and citalopram. Nonetheless, the Ki values suggest that all three drugs have moderate potency toward human AChE. Data are given as mean ± SD. The nonlinear regression analyses were done with GraphPad Prism 9.
