Tan Tan Sun

RAPID AND MILD SYNTHESES OF RADIOIODINATED ESTROGEN DERIVATIVES VIA ORGANOBORANE TECHNOLOGY

Abstract Radioiodinated estrogen derivatives of potential use as receptor-binding agents have been synthesized via the reaction of organoboranes with 125 ICl, The utility of organoboranes as intermediates in radiopharmaceutical syntheses is discussed.

Comparison of 68Ga-EDTA, [l-11C]α-aminoisobutyric acid, and [99mTC]sodium pertechnetate in an experimental blood-brain barrier lesion

Unilateral opening of the blood-brain barrier (BBB) in rats, induced by infusion of a hyperosmotic solution of mannitol into the left internal carotid artery, was applied to compare 68Ga-EDTA, [1-11C]alpha-aminoisobutyric acid (using the long-lived 14C-labeled analog), and [9mTc]sodium pertechnetate as agents for diagnosis of BBB disruption. Of the three agents and two time intervals studied, 68Ga-EDTA at 30 min postinjection gave the highest target-to-nontarget ratio. In addition, 68Ga-EDTA, unlike commonly used [99mTc]sodium pertechnetate, can be used in conjunction with positron emission tomography, which could make possible earlier and better assessment of BBB defects using 68Ga-EDTA.