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

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.

Graphical abstractMicroPET image 60 min 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).Figure optionsDownload full-size imageDownload as PowerPoint slide