Compositions useful for labeling .beta.-amyloid plaques and
neurofibrillary tangles are provided. The compositions comprises
compounds of formula (I): ##STR00001## wherein R.sub.1 is selected from
the group consisting of --C(O)-alkyl, --C(O)-alkylenyl-R.sub.4,
--C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4, --C.dbd.C(CN).sub.2-alkyl,
--C.dbd.C(CN).sub.2-alkylenyl-R.sub.4, ##STR00002## wherein R.sub.4 is a
radical selected from the group consisting of alkyl, substituted alkyl,
aryl and substituted aryl; R.sub.5 is a radical selected from the group
consisting of --NH.sub.2, --OH, --SH, --NH-alkyl, --NHR.sub.4,
--NH-alkylenyl-R.sub.4, --O-alkyl, --O-alkylenyl-R.sub.4, --S-alkyl, and
--S-alkylenyl-R.sub.4; R.sub.6 is a radical selected from the group
consisting of --CN, --COOH, --C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4,
--C(O)-alkyl, --C(O)-alkylenyl-R.sub.4, --C(O)-halogen, --C(O)NH-alkyl,
--C(O)NH-alkylenyl-R.sub.4 and --C(O)NH.sub.2; R.sub.7 is a radical
selected from the group consisting of O, NH, and S; and R.sub.8 is N, O
or S; and R.sub.2 is selected from the group consisting of alkyl and
alkylenyl-R.sub.10 and R.sub.3 is alkylenyl-R.sub.10, wherein R.sub.10 is
selected from the group consisting of --OH, --OTs, halogen, spiperone,
spiperone ketal, and spiperone-3-yl, or R.sub.2 and R.sub.3 together form
a heterocyclic ring, optionally substituted with at least one radical
selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen,
alkyl-R.sub.10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl,
and further wherein one or more of the hydrogen, halogen or carbon atoms
are optionally replaced with a radiolabel.