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Thus, based on the abovementioned characteristics of 18F-MK-9470, we expect no unspecific binding of this tracer in bone metastases.
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An intravenous injection of about 185 MBq was administered and the images were acquired 3 4 h after injection on a multidetector or multiheaded γ camera with LEHR collimators, a time point at which the specific binding ratio of this tracer to the DAT is stable.
Two mechanisms were assessed: binding of the tracer to melanin or to sigma receptors of melanoma cells.
The autoradiograms presented binding of the tracer to the tumor sections.
Non-specific binding of the tracer in the tissue can slow down the association rate of the tracer-receptor binding by leaving less free tracer in the tissue.
Relatively low receptor affinity could lead to low binding potential, which results from substantial binding of the tracer to other parts of the body.
Pretreatment of the tumor sections with ALK5 blocking agents EW-71977, SB-431542 and the ALK5 inhibitor) decreased the binding of the tracer significantly.
A prediction of the target-bound fraction of tracer (ftb) was made from measurements of target affinity, density, and the non-specific binding of the tracer measured in brain slices.
Especially, the high plasma protein binding of the tracer, which results in slow clearance kinetics and high blood pool activity can interfere with the detection of lower avidity or smaller tumor lesions [7, 8].
However, these positive characteristics, which indicate the specific binding of the tracer to α7 nAChRs, were diminished by the fact that these compounds also showed the same levels of blocking in the cerebellum.
Kinetic modeling based on dynamic PET scans suggested specific binding of the tracer.
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com