Design of bifunctional radiopharmaceutical for the development of 99mTc complexes for myocardial imaging agents.
Several bifunctional radiopharmaceuticals (BR), molecules containing a neutral 99mTc-dithiosemicarbazone (DTS) structure as a chelating site, along with a functional amino group (primary tertiary and quaternary amino group) are tested for their chemical or biological functionalities as myocardial agents. Investigation of these amino compounds is carried out in vitro and in vivo. Mice (ddY) distribution studies show a high radioactivity distribution in heart with every tested derivative, but the highest heart to blood ratio of 2.92 (1 h) is achieved with the quaternary amino DTS. Also, this derivative displays low lung uptake inducing a proper target/non-target ratio for myocardial agent. The role conveyed by the various amino containing side chain in the biodistribution and validity of DTS derivative as BR are discussed.
D000818:Animals; D006321:Heart / Q000000981:diagnostic imaging*; D051379:Mice; D008815:Mice, Inbred Strains; D009206:Myocardium / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000378:metabolism; D011877:Radionuclide Imaging; D013667:Technetium / Q000378:metabolism; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000378:metabolism; D014018:Tissue Distribution
D009942:Organometallic Compounds; D013882:Thiosemicarbazones; C015848:dithiosemicarbazone; D013667:Technetium