A suitable method to monitor inhibition of cholinesterase activities in tissues as induced by reversible enzyme inhibitors.
A radiometric method has been used to estimate in vivo activities of cholinesterases in various tissues in the presence of reversible inhibitors. Determination of the samples was performed with the lowest possible degree of dilution to avoid reactivation of the enzyme which would prevent reliable calculation. Dose-response curves and concentration-response curves were performed using physostigmine and tetrahydroacridine, two reversible anticholinesterases in clinical use. Specific inhibition of acetyl- and butyrylcholinesterase was performed using BW284C51 and iso-OMPA, respectively.
Thomsen
T
T
Institut für Klinische Pharmakologie, Klinikum Steglitz, Freie Universität Berlin.
Kewitz
H
H
Pleul
O
O
D000110:Acetylcholinesterase / Q000097:blood / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000201:enzymology; D002091:Butyrylcholinesterase / Q000097:blood / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000032:analysis* / Q000378:metabolism / Q000494:pharmacology; D002802:Cholinesterases / Q000378:metabolism*; D007457:Iodine Radioisotopes; D007700:Kinetics; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011865:Radioisotope Dilution Technique
D002800:Cholinesterase Inhibitors; D007457:Iodine Radioisotopes; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002802:Cholinesterases