Abstract:
INTRODUCTION:Severe brain hypoxia in the territory of the occluded artery is a key feature of ischemic stroke. This region can be imaged using positron emission tomography (PET) and the standard hypoxia radiotracer (18)F-fluoromisonidazole ((18)F-FMISO). However, the utility of (18)F-FMISO is limited by its slow accumulation in the lesion. Therefore, this study investigated three hypoxia-sensitive radiotracers, namely the nitroimidazole (18)F-fluoroazomycin arabinoside ((18)F-FAZA) and two (64)Cu bis(thiosemicarbazone) complexes ((64)Cu-ATSM and (64)Cu-ATSE), expected to have improved pharmacokinetic profiles relative to (18)F-FMISO, in a rodent model of ischemic stroke. METHODS:In anaesthetised Wistar rats, the distal middle cerebral artery was permanently occluded by electrocoagulation, the radiotracers administered intravenously and animals PET scanned for up to 3hours, followed by T2-weighted magnetic resonance imaging to map the infarct. RESULTS:As expected, late and prominent (18)F-FMISO retention was observed despite lower tracer delivery into the affected region. Time-activity curves revealed that both (64)Cu-ATSM and (64)Cu-ATSE showed rapid entry and efflux from the brain, but did not show significant accumulation in the lesion. (18)F-FAZA showed limited brain penetration, and accumulation in the lesion was inconsistent, low and as slow as (18)F-FMISO. CONCLUSIONS:This study suggests further development of these radiotracers as hypoxia markers for ischemic stroke may not be warranted.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Williamson DJ,Ejaz S,Sitnikov S,Fryer TD,Sawiak SJ,Burke P,Baron JC,Aigbirhio FIdoi
10.1016/j.nucmedbio.2012.11.012subject
Has Abstractpub_date
2013-04-01 00:00:00pages
338-44issue
3eissn
0969-8051issn
1872-9614pii
S0969-8051(12)00309-5journal_volume
40pub_type
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