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Tissue Distribution of High-Density Lipoprotein Labeled with Radioiodinated Cholesterol

University of Michigan Medical School, Ann Arbor, Michigan

Correspondence: For reprints contact: R. E. Counsell, PhD, Dept. of Pharmacology, Univ. of Michigan Medical School, Ann Arbor, MI 48109.

ABSTRACT

This preliminary study was undertaken in order to explore possible methods for enhancing the target organ specificity of radioiodinated cholesterol. 19-[¹²⁵I]cholesterol (I*C) was rapidly incorporated and transported in high-density lipoproteins (HDL) following i.v. administration to rats, and thus behaved like cholesterol in this regard. Incorporation of I*C into HDL (I*C-HDL) before administration produced little change in the tissue distribution profile except for a reduction in the amount of radioactivity appearing in the thyroid. This suggested that the lipoprotein carrier may have afforded protection from metabolic dehalogenation of I*C. When rats were pretreated with 4-aminopyrazolo-(3,4d)-pyrimidine to drastically reduce the circulating lipoprotein levels, a fourfold enhancement in adrenal uptake was observed following administration of I*C-HDL. This finding was consistent with the current view that the rat adrenal contains high-affinity and saturable receptors for HDL.