Inactivation of acetylcholinesterase by various fluorophores

Figures & data

Figure 1.  The chemical structures of the fluorophore amides.

Table 1.  Inhibition of rMAChE and EEAChE (IC₅₀ μM; n = 3) by fluorophore amides 4, 6, and 7. Amides 1–3, 5 were inactive at ≥50 μM.

	4	6	7
rMAChE	1.00 ± 0.47 Activity	0.05 ± 0.02	0.70 ± 0.08
EEAChE	>50	3.57 ± 1.45	10.4 ± 2.1

Figure 2.  Double reciprocal Lineweaver–Burk plot showing the inhibition of EEAChE by Lissamine propargylsulfonamide 6. Inset A: determination of K_i for Lissamine propargylsulfonamide 6 using a plot of the slopes versus inhibitor concentration. y = 0.0446x + 0.523; R² = 0.996. Inset B: determination of K_i′ for Lissamine propargylsulfonamide 6 using a replot of the intercepts versus inhibitor concentration. y = 108.9x + 2.717; R² = 0.995.