Synthesis, I-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with a Tributylstannyl Prosthetic Group in Their Structures.

Prostate-specific membrane antigen (PSMA) has been identified as a target for the development of theranostic agents. In our current work, we describe the design and synthesis of novel N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-L-lysine (DCL) urea-based PSMA inhibitors with a chlorine-substituted aromatic fragment at the lysine ε-nitrogen atom, a dipeptide including two phenylalanine residues in the L-configuration as the peptide fragment of the linker, and 3- or 4-(tributylstannyl)benzoic acid as a prosthetic group in their structures for radiolabeling. The standard compounds [I]PSMA-m-IB and [I]PSMA-p-IB for comparative and characterization studies were first synthesized using two alternative synthetic approaches.

Radiolabeled Complex of Antimicrobial Peptides UBI29-41 and UBI18-35 Labeled with Tc for Differential Diagnosis of Bone Infection of the Limbs.

We studied an original radiolabeled complex of antimicrobial peptides UBI29-41 and UBI18-35, ubiquicidin derivatives, for distinguishing between bacterial and aseptic inflammation. For radiolabeling of the peptides with technetium-99m, a bifunctional chelating agent succinimide-1-yl 6-(bis(pyridin-2-ylmethyl)amino)hexanoate was used. The obtained complexes Тс-DPAH-UBI29-41 and Тс-DPAH-UBI18-35 had radiolabeling yield >80% and radiochemical purity >96%.

Tc-labeled nanocolloid drugs: development methods.

The work considers the problem of obtaining nanocolloid radiopharmaceuticals (RPs) and studying their functional suitability for diagnosing sentinel lymph nodes (SLN) in cancer patients. Two principal approaches to the formation of technetium-99m-labeled particles based on inorganic and organic matrices were considered when carrying out research to develop methods for the production of nanocolloid RPs. The composition of the reagents and the conditions for obtaining nanocolloid radiopharmaceuticals were determined.

Tc-labeled monosaccharide kits: development methods and quality control.

The paper presents the procedure for planning an experiment to create standard sets of reagents for a technetium-99m generator based on glucose derivatives. All stages are presented from researching the required quantities of a substance, a reducing agent, a stabilizer and auxiliary components to developing lyophilized kits and conducting quality control. The radiochemical purity of radiopharmaceuticals prepared on the basis of the developed kits ranged from 90.