Biodistribution of model 105Rh-labeled tetradentate thiamacrocycles in rats.
105Rh(III)Cl2 complexes with a limited series of [14]ane- and [16]ane- thia macrocycles were prepared and their biodistributions in Sprague-Dawley rats studied. These studies demonstrate that modifications in the structure and composition of the 105Rh-thia macrocycle complexes produce significant differences in their uptake and retention in both the liver and kidneys. The results indicate that the cis-Rh(III)Cl2-[14]ane thiamacrocycles exhibit less kidney retention than the corresponding trans-Rh(III)Cl2-[16]ane thiamacrocycles. In addition, the presence of a side chain containing a carboxylate group will produce decreased retention of activity in the kidneys. HPLC analysis of urine from these animals indicates no observable in vivo metabolism or dissociation of these chelates in the blood stream.
Li
N
N
Department of Radiology and Chemistry, University of Missouri, Columbia 65211, USA.
Struttman
M
M
Higginbotham
C
C
Grall
A J
AJ
Skerlj
J F
JF
Vollano
J F
JF
Bridger
S A
SA
Ochrymowycz
L A
LA
Ketring
A R
AR
Abrams
M J
MJ
Volkert
W A
WA
D000818:Animals; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D008024:Ligands; D011868:Radioisotopes; D051381:Rats; D017207:Rats, Sprague-Dawley; D012238:Rhodium; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
D006571:Heterocyclic Compounds; D008024:Ligands; D011868:Radioisotopes; D012238:Rhodium