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. 2014 Oct 22;40(3):755–765. doi: 10.1038/npp.2014.245

Figure 2.

Figure 2

VU0092273 displays dose-dependent in vivo receptor occupancy (RO) of the mGlu5 (metabotropic glutamate receptor subtype 5) MPEP (methyl-6-(phenylethynyl)pyridine hydrochloride) site. (a) Positron emission tomography representative images of [18F]FPEB binding in vehicle-, VU0092273-, VU0360172-, and MTEP-treated rat brains. (b) Pretreatment with VU0092273 (3–100 mg/kg, i.p.) dose-dependently displaces [18F]FPEB binding in the striatum with an ED50 of 17.3 mg/kg and maximum percent occupancy of 80.1±8. (c) In addition, VU0360172 does not significantly displace [18F]FPEB binding to mGlu5 in vivo, demonstrating that RO does not predict in vivo efficacy for this mGlu5 PAM. Time-activity curve of [18F]FPEB binding in the cerebellum and striatum following vehicle and VU0360172 (100 mg/kg, 30 min, i.p.). Data represent mean standard uptake value±SEM (n=5–7).