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Background  Metabotropic glutamate 7 (mGlu7) receptor is a crucial target protein for the development of pharmaceuticals against central nervous system disorders. In the present study, we synthesized [ 11 C]MMPIP, a putative radioligand for mGlu7 (binding constant  K  B  = 30 nM), and evaluated its potential for imaging of mGlu7 via  in vitro  and  in vivo  techniques.    Methods  [ 11 C]MMPIP was synthesized by the reaction of phenol precursor  3  with [ 11 C]CH 3 I.  In vitro  autoradiography using [ 11 C]MMPIP was performed on rat brain sections. To determine  in vitro  specific binding of [ 11 C]MMPIP with mGlu7, a blocking study was conducted by co-incubation with excess AMN082, a selective antagonist for mGlu7, or unlabeled MMPIP. Positron emission tomography (PET) studies and  ex vivo  metabolite analysis were carried out on rat brains.    Results  [ 11 C]MMPIP was obtained with two specific activity (SA) levels of average 58 (conventional) and 3,800 (high SA) GBq/μmol, respectively. High radioactive signals derived from conventional [ 11 C]MMPIP in the  in vitro  autoradiography were seen in the thalamus, medulla oblongata, and striatum, corresponding with comprehensive brain distributions of mGlu7. Co-incubation with ANM082 or unlabeled MMPIP reduced the radioactive signals in the brain sections, respectively. In the PET studies with [ 11 C]MMPIP, no specific uptake relative to mGlu7 was found in the examined brain regions.    Conclusion  Despite  in vitro  specific binding of [ 11 C]MMPIP with mGlu7, visualization of mGlu7 in the living brain using PET was not successful. Development of new ligand candidates with higher affinity for mGlu7 is necessary.

Synthesis and evaluation of [11C]MMPIP as a potential radioligand for imaging of metabotropic glutamate 7 receptor in the brain