Evaluation of phenylmethanesulfonyl fluoride (PMSF) as a tracer candidate mapping acetylcholinesterase in vivo.
The availability of phenylmethanesulfonyl fluoride (PMSF), an irreversible cholinesterase inhibitor, for a tracer mapping acetylcholinesterase (AchE) in vivo in brain and other organs was evaluated using [35S]PMSF in mice and rats. [35S]PMSF was well taken up into the brain, heart and muscle, and the radioactivities were trapped in these organs. Pretreatment with non-labeled PMSF decreased 33-40% of the trapped radioactivities in the brain and other organs in mice. However, regional distribution of [35S]PMSF in rat brain did not correlate well with that of AchE activity, suggesting that the selectivity of PMSF toward AchE may be insufficient for use as an in vivo tracer mapping AchE.
Irie
T
T
Division of Clinical Research, National Institute of Radiological Sciences, Chiba, Japan.
Fukushi
K
K
Iyo
M
M
D000110:Acetylcholinesterase / Q000032:analysis* / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000201:enzymology* / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D005069:Evaluation Studies as Topic; D008297:Male; D051379:Mice; D008809:Mice, Inbred C3H; D010664:Phenylmethylsulfonyl Fluoride / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013462:Sulfur Radioisotopes
D002800:Cholinesterase Inhibitors; D013462:Sulfur Radioisotopes; D010664:Phenylmethylsulfonyl Fluoride; D000110:Acetylcholinesterase