title: 99mTc-labeled vasopressin peptide as a radiopharmaceutical for small-cell lung cancer (SCLC) diagnosis.
abstract: The 99mTc-labeled conjugates of the vasopressin (AVP) peptide and of its analogue d(CH2)5[D-Tyr(Et2)-Ile4-Eda9]AVP (AVP(an)) have been synthesized using the technetium complexes with tetradentate tripodal chelator (the tris(2-mercaptoethyl)amine (NS3)) and the monodentate isocyanide ligand (CN-peptide). The conjugates exhibit high stability in the presence of 100 times the molar excess of standard amino acids cysteine or histidine and also satisfactory stability in human serum. The 99mTc(NS3)(CN-AVP) and 99mTc(NS3)(CN-AVP(an)) ability of binding to small-cell lung cancer (SCLC) cell line H69 was studied in vitro. The results suggest that the novel vasopressin conjugate 99mTc(NS3)(CN-AVP(an)) is a desirable compound for imaging oncogene receptors overexpressed in SCLC cells and can be an important basis for further consideration the conjugate as a potential diagnostic radiopharmaceutical for patients suffering from small-cell lung cancer.
authors: Centre for Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology , Dorodna 16, 03-195 Warsaw, Poland.
authors: Ewa
authors: E
authors: Gniazdowska
authors: Przemysław
authors: P
authors: Koźmiński
authors: Krzysztof
authors: K
authors: Bańkowski
authors: Paweł
authors: P
authors: Ochman
mesh_terms: D000818:Animals; D002289:Carcinoma, Non-Small-Cell Lung / Q000175:diagnosis*; D006801:Humans; D008175:Lung Neoplasms / Q000175:diagnosis*; D008968:Molecular Conformation; D009842:Oligopeptides / Q000097:blood / Q000737:chemistry; D009942:Organometallic Compounds / Q000097:blood / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000097:blood / Q000737:chemistry; D051381:Rats; D012211:Rhenium / Q000097:blood / Q000737:chemistry; D013667:Technetium / Q000097:blood / Q000737:chemistry; D014407:Tumor Cells, Cultured; D014667:Vasopressins / Q000097:blood / Q000737:chemistry
chemical_list: D009842:Oligopeptides; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D014667:Vasopressins; D012211:Rhenium; D013667:Technetium