| 3939750 |
Lindgren B, Lindgren G, Artursson E, Puu G: Acetylcholinesterase inhibition by sulphur and selenium heterosubstituted isomers of N,N-diethylcarbamyl choline and carbaryl. J Enzyme Inhib. 1985;1(1):1-11.
Nine sulphur and selenium heterosubstituted isomers of N,N-diethylcarbamylcholine and carbaryl have been prepared and their inhibiting activity towards electric eel acetylcholinesterase (E.C. 3.1.1.7) have been measured. The N,N-diethylcarbamylcholines acted only as reversible inhibitors, i.e. they could not carbamylate the enzyme. The reversible inhibition was of mixed type. Sulphur and selenium substitution had only marginal effects on Ki (0.2-0.3 mM) but reduced the value of K'i. The heterosubstituted carbaryl analogues were, with one exception, found to be irreversible inhibitors, about 100 times less potent than carbaryl. |
162(2,2,2,2) |