Estimation of plasma tacrine concentrations using an in vitro cholinesterase inhibition assay.
THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. In this study, a sensitive radiometric assay for THA inhibition of human plasma ChE, suitable for detection of effects of orally administered drug, is described. The assay is sensitive in a range of 4-50 ng/ml plasma. Reversibility of the inhibition permits distinguishing of drug effects on ChE from changes in amount of enzyme synthesized during treatment.
Moriearty
P L
PL
Department of Psychiatry, Southern Illinois University School of Medicine, Springfield 62794-9230.
Kenny
W
W
Kumar
V
V
D000284:Administration, Oral; D000609:Aminoacridines / Q000097:blood*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D002802:Cholinesterases / Q000097:blood; D006801:Humans; D009994:Osmolar Concentration; D011874:Radiometry / Q000379:methods*; D013619:Tacrine / Q000097:blood* / Q000494:pharmacology
D000609:Aminoacridines; D002800:Cholinesterase Inhibitors; D013619:Tacrine; D002802:Cholinesterases