Mitochondrial Avid Radioprobes. Preparation and Evaluation of7'(Z)-[125I]Iodorotenone and 7'(Z)-[125I]Iodorotenol Page: 2 of 26
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The loss of mitochondrial function has been implicated in a number of maladies such as
Huntington's Disease, Parkinson's Disease, cancer and cardiovascular disease. The objective of
this research was to develop a radiolabeled mitochondrial probe. Two tracers, 7'-Z-iodorotenol
and 7'-Z-iodorotenone, analogs of rotenone a natural product that inhibits Complex I of the
mitochondrial electron transport chain, have been labeled with iodine-125 in 45-85% yield in a
single step from the corresponding tribuytylstannyl precursor. In vivo distribution in adult male
Sprague-Dawley rats for both compounds showed high accumulation in the heart (1.7-3.7 %ID/g
at lh), a tissue with high mitochondrial content. Z-Iodorotenol did not washout of most tissues
between 1 and 2 h post injection whereas Z-iodorotenone showed moderate washout (7-26%)
over the same period. By 24 h there was significant loss of both compounds from most tissues
including the heart. Heart-to-blood, -lung and -liver ratios for Z-iodorotenone of 28.9, 10.7 and
2.4, respectively, were two- to four-fold higher than the Z-iodorotenol ratios. Compared to the
current clinical perfusion tracers, 99mTc-sestamibi and 99mTc-tetrofosmin, Z-iodorotenone
demonstrates similar lh heart accumulation and significantly higher heart-to-lung ratio (P
<0.001). Z-Iodorotenone heart-to-liver ratio is equivalent to 99mTc-sestamibi. 7'-Z-Iodorotenone
possesses distribution characteristics of an improved tracer for SPECT perfusion studies.
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VanBrocklin, Henry F.; Hanrahan, Stephen M.; Enas, Joel D.; Nandanan, Erathodiyil & O'Neil, James P. Mitochondrial Avid Radioprobes. Preparation and Evaluation of7'(Z)-[125I]Iodorotenone and 7'(Z)-[125I]Iodorotenol, article, October 18, 2006; Berkeley, California. (digital.library.unt.edu/ark:/67531/metadc897429/m1/2/: accessed September 19, 2018), University of North Texas Libraries, Digital Library, digital.library.unt.edu; crediting UNT Libraries Government Documents Department.