Inhibition of acetylcholinesterase by 3-methoxy catecholamine derivatives

Methoxy-catecholamine excretion and the mecholyl test.

THE response of systolic blood pressure to the subcutaneous injection of mecholyl has been studied repeatedly as a correlate of psychopathological state since the initial report of MYERSON.~ In 1948, FUNKENSTEIN et ~1.~ standardized a test using the response of systolic blood pressure to epinephrine and to mecholyl, and correlated these response patterns with the outcome following electroconvul...

Carbamyl derivatives of acetylcholinesterase.

It has recently been shown that carbamyl derivatives of acetylcholinesterase can be obtained by the reaction of the enzyme with dimethylcarbamyl fluoride, dimethylcarbamyl choline, and carbamyl choline (1). These substances inhibit the enzyme slowly and once inhibited, the enzyme recovers activity slowly upon dilution. The rate of recovery is the same when the inhibitor is either dimethylcarbam...

Inhibition of acetylcholinesterase by two genistein derivatives: kinetic analysis, molecular docking and molecular dynamics simulation

In this study two genistein derivatives (G1 and G2) are reported as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), and differences in the inhibition of AChE are described. Although they differ in structure by a single methyl group, the inhibitory effect of G1 (IC50=264 nmol/L) on AChE was 80 times stronger than that of G2 (IC50=21,210 nmol/L). Enzyme-kinetic analys...

inhibition of the p300 histone acetyl transferase by 3-(2h) isothiazolones and analogous oxazolidinone derivatives

Characterization of acetylcholinesterase-inhibition by itopride.

Itopride is a gastroprokinetic benzamide derivative. This agent inhibited both electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BuChE). The IC50 of itopride with AChE (2.04 +/- 0.27 microM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3 +/- 3.4 nM), it was 10-fold less. The recovery of AChE activity inhibited b...