Novel polar single amino acid chelates for technetium-99m tricarbonyl-based radiopharmaceuticals with enhanced renal clearance: application to octreotide.

摘要: Single amino acid chelate (SAAC) systems for the incorporation of M(CO)3 moiety (M = Tc/Re) have been successfully incorporated into novel synthetic strategies radiopharmaceuticals and evaluated in a variety biological applications. However, lipophilicity first generation Tc(CO)3-dipyridyl complexes has resulted substantial hepatobiliary uptake when either examined as lysine derivatives or integrated biologically active small molecules peptides. Here we designed, synthesized, SAAC that chemically modified to promote overall Tc(CO)3L3 complex hydrophilicity with intent enhancing renal clearance. A series derived containing functionalized polar imidazole rings and/or carboxylic acids were synthesized via reductive alkylation e group lysine. The radiolabeled 99mTc, purified, radiochemical stability, lipophilicity, tissue distribution rats. l...