Mitochondrial Avid Radioprobes. Preparation and Evaluation of7'(Z)-[125I]Iodorotenone and 7'(Z)-[125I]Iodorotenol Page: 2 of 26
This article is part of the collection entitled: Office of Scientific & Technical Information Technical Reports and was provided to Digital Library by the UNT Libraries Government Documents Department.
The following text was automatically extracted from the image on this page using optical character recognition software:
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.
Here’s what’s next.
This article can be searched. Note: Results may vary based on the legibility of text within the document.
Tools / Downloads
Get a copy of this page or view the extracted text.
Citing and Sharing
Basic information for referencing this web page. We also provide extended guidance on usage rights, references, copying or embedding.
Reference the current page of this Article.
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 December 19, 2018), University of North Texas Libraries, Digital Library, digital.library.unt.edu; crediting UNT Libraries Government Documents Department.