Pancreatic receptors: initial feasibility studies with a targeted contrast agent for MR imaging

To evaluate cholecystokinin (CCK) as a target-specific vector for magnetic resonance (MR) receptor imaging of rat pancreas.

Monocrystalline iron oxide (MION) was labeled with CCK by noncovalent attachment. Receptor specificity of the conjugate was determined with competitive binding studies. Pharmacologic determinations were blood half-lives, biodistribution, time responses, dose responses, and limited toxicity.

Specific cell binding of MION-20-CCK was saturable and inhibitable by a CCK antagonist. Blood half-life of MION-20-CCK was 20 minutes, which was shorter than that of unlabeled MION. Biodistribution studies showed a statistically significant decrease in relaxation times in pancreatic tissues from 42.7 msec +/- 2.0 to 33.8 msec +/- 1.4 (P < or = .05) but not in tumor after administration of MION-20-CCK. The half-life of MION-20-CCK in the pancreas was 3 weeks; no signs of toxicity were shown at the level tested.

Target-specific MR imaging of pancreatic receptors is feasible. Additional studies are necessary to perfect binding strategies, optimize preparations, and scale up synthesis for imaging in other species.