Table 2.
Inhibition of carboxylesterases by cholinesterase inhibitors.
Inhibitor | IC50 (μM) | |||
---|---|---|---|---|
hCE1 | hiCE | AChE | BChE | |
Benzil | 0.37 ± 0.04 | 0.33 ± 0.03 | >100 | >100 |
Tolserine | >100 | >100 | 1.4 ± 0.1 | 53.1 ± 20.1 |
Phenethylcymserine | 20.5 ± 10.4 | 5.6 ± 2.7 | 1.0 ± 0.2 | 0.51 ± 0.06 |
Donepezil | >100 | >100 | 0.022 ± 0.005 | 7.6 ± 1.3 |
Tacrine | >100 | >100 | 0.079 ± 0.002 | 0.034 ± 0.001 |
Rivastigmine | >100 | >100 | 299 ± 24.6 | 280 ± 110 |
Galantamine | >100 | >100 | 1.2 ± 0.4 | 21.7 ± 4.3 |
Bis(7)-tacrine | 40.5 ± 22.0 | 23.7 ± 3.5 | 0.0011 ± 0.0001 | 0.033 ± 0.003 |
Acridine | >100 | >100 | 252 ± 80.9 | 6.9 ± 1.4 |
ACMA | 111 ± 54.5 | 28.4 ± 11.4 | 2.0 ± 0.2 | 2.5 ± 0.9 |
DEA | 99.3 ± 32.0 | 41.6 ± 15.2 | 6.9 ± 0.7 | 2.4 ± 0.5 |