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Background  A recent study from our laboratory demonstrated that  11 C-LY2428703, a new positron emission tomographic radioligand for metabotropic glutamate receptor 1 (mGluR1), has promising  in vitro  properties and excellent  in vivo  performance for imaging rat brain. The present study evaluated  11 C-LY2428703 for imaging mGluR1 in monkey and human brains.    Methods  Rhesus monkeys were imaged at baseline and after administration of an mGluR1 blocking agent to calculate nonspecific binding, as well as after the administration of permeability glycoprotein (P-gp) and breast cancer resistance protein (BCRP) blockers to assess whether  11 C-LY2428703 is a substrate for efflux transporters at the blood–brain barrier. Human imaging was performed at baseline in three healthy volunteers, and arterial input function was measured.    Results  Overall brain uptake was low in monkeys, though slightly higher in the cerebellum, where mGluR1s are concentrated. However, the uptake was not clearly displaceable in the scans after mGluR1 blockade. Brain penetration of the ligand did not increase after P-gp and BCRP blockade. Brain uptake was similarly low in all human subjects (mean  V  T  with a two-tissue compartment model, 0.093 ± 0.012 mL/cm 3 ) and for all regions, including the cerebellum.    Conclusions  Despite promising  in vitro  and  in vivo  results in rodents,  11 C-LY2428703 was unsuitable for imaging mGluR1s in monkey or human brain because of low brain uptake, which was likely caused by high binding to plasma proteins.

ejnmmi research

11C-LY2428703, a positron emission tomographic radioligand for the metabotropic glutamate receptor 1, is unsuitable for imaging in monkey and human brains