REAGENTS FOR ASSAYING CENTRAL LOCAL ACETYLCHOLINESTERASE ACTIVITY

摘要

N-alkylpideridine dervatives represented by general formula (1) or (2); reagents containing the same for assaying central local AchE activity; a method of assaying the central local AchE activity; and labeled precursors of the above compounds, wherein R 1 represents optinally fluorinated lower alkyl; R 2 represents lower alkyl; and R 3 represents alkenyl substituted at the 1-position by hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyl-oxyalkyloxy or lower alkanoyloxy and at the end by radioactive iodine, or alkenyloxymethyl substituted at the end by radioactive iodine. After easily passing through the cerabral blood barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols and then captured by the brain. The alcohols formed in the brain do not migrate into the brain. At the same time, they emit gamma-ray at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.