Cell adhesion mols., such as integrins, play a vital role in angiogenesis, a key pathway for tumor growth, invasion and metastasis.The integrin αvβ3, which recognizes the RGD sequence (Arg-Gly-Asp), may provide a target for in vivo tumor imaging.A linear and a cyclic RGD peptide derivative (RGDfK-His and cRGDfK-His, resp.), labeled via the precursor [99mTc(H2O)3(CO)3]+, were comparatively evaluated and their radiobiol. properties were assessed in normal and tumor-bearing mice.Biodistribution studies showed non-specific uptake in all organs, rapid blood clearance and elimination via the hepatobiliary and urinary systems.Tumor uptake was higher for the cyclic radiolabeled derivative, as both biodistribution and imaging studies suggested.The cRGDfK-His, labeled via the fac-[99mTc(CO)3]-core, may prove to be a useful tool for early tumor detection.