Synthesis and biological evaluation of 68Ga labeled bis-DOTA-3,3′-(benzylidene)-bis-(1H-indole-2-carbohydrazide) as a PET tracer for in vivo visualization of necrosis
MicroPET image 60min pi of 68Ga-bis-DOTA-BI of a Wistar rat with a reperfused partial liver infarction in transverse (left), coronal (middle) and sagittal (right) views. Besides the kidneys (K), a clear uptake can be seen in the right necrotic liver lobes (arrow). The aim of the present study was to...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2013-06, Vol.23 (11), p.3216-3220 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | MicroPET image 60min pi of 68Ga-bis-DOTA-BI of a Wistar rat with a reperfused partial liver infarction in transverse (left), coronal (middle) and sagittal (right) views. Besides the kidneys (K), a clear uptake can be seen in the right necrotic liver lobes (arrow).
The aim of the present study was to develop a 68Ga labeled bis-DOTA derivative of benzylidene-bis-indole and compare the in vivo stability and biodistribution with that of the previously reported bis-DTPA derivate for in vivo imaging of necrosis using PET. Uptake of the tracer was evaluated in a mouse model of Fas-mediated hepatic apoptosis in correlation with histochemical stainings. The novel 68Ga labeled tracer showed an improved in vivo stability and could therefore be used for selective non-invasive imaging of necrotic cell death using PET. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2013.03.127 |