We have synthesized and investigated 8 peptidyl-cyclodextrin adducts in ord
er to validate the general concept of drug-targeting. The adducts are compo
sed of a beta- or gamma-cyclodextrin part and a peptidic moiety consisting
of the neuropeptide Substance P or one of its shorter derivatives, Substanc
e P4-11. All these new compounds were fully characterized by dedicated NMR
experiments and by mass spectrometry. The inclusion properties of the cyclo
dextrin moiety were also preserved as demonstrated by NMR experiments. Anti
bodies raised against beta-, gamma-cyclodextrin and Substance P, respective
ly, recognized the corresponding moiety in all prepared peptidyl-cyclodextr
in derivatives.