Abstract:
:Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecular weight. The biodistribution of these complexes was determined in normal mice, and several of the complexes selectively accumulated in the lungs as compared to the liver or other organs. Pulmonary accumulation varied greatly with subtle changes in structure, and a 30-fold range of lung uptake (1-31% of the injected dose/organ) was observed for isomeric technetium complexes which have identical molecular weights and similar log PC. Further, a parabolic relationship between lung uptake and log PC was observed for a subset of the complexes which are derived from a homologous series of tetramethyl-DADT ligands. Neutral and lipophilic radiopharmaceuticals labeled with technetium can therefore be developed which exhibit structurally specific uptake in the lung.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Lever SZ,Sun SY,Scheffel UA,Kaltovich FA,Baidoo KE,Goldfarb H,Wagner HN Jrdoi
10.1002/jps.2600830609subject
Has Abstractpub_date
1994-06-01 00:00:00pages
802-9issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49491-2journal_volume
83pub_type
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