Potential tumor- or organ-imaging agents. 28. Radioiodinated esters of cholesterol and pregnenolone.
Previous studies had shown radioiodinated esters of cholesterol and pregnenolone to accumulate in steroid-secreting tissues of the rat. This was particularly true for radioiodinated iopanoate esters. The present study was undertaken to examine the effect of the iopanoyl amino group on the tissue distribution of these esters. While the tissue distribution profiles for cholesteryl iopanoate and the desamino analog (III) were somewhat comparable, such was not the case for the corresponding esters of pregnenolone. Moreover, this subtle structural change of removing the amino group was observed to affect the in vivo stability of the esters to hydrolysis. This conclusion is in accordance with the observation that the tissue distribution profiles for the free acids I and II are not significantly different from each other. These studies serve to demonstrate that relatively minor modifications of the acyl moiety have a profound effect on both the uptake and distribution of these sterol esters in various tissues.
Van Dort
M
M
Department of Pharmacology, University of Michigan Medical School, Ann Arbor 48109.
Schwendner
S W
SW
Counsell
R E
RE
D000818:Animals; D001693:Biological Transport, Active; D002788:Cholesterol Esters / Q000493:pharmacokinetics*; D004952:Esters; D005260:Female; D007457:Iodine Radioisotopes; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging; D011284:Pregnenolone / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D051381:Rats; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
D002788:Cholesterol Esters; D004952:Esters; D007457:Iodine Radioisotopes; D011284:Pregnenolone