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. Author manuscript; available in PMC: 2022 Jan 12.
Published in final edited form as: ACS Chem Neurosci. 2019 Oct 28;10(11):4558–4570. doi: 10.1021/acschemneuro.9b00415

Table 3.

Summary of IC50 Values of Various mGlu5 NAMs in mGlu5/HEK Cells and Striatal, Hippocampal, and Cortical Culturesa

IC50
NAM mGlu5 HEK striatal hippocampal cortical
MPEP 42.4 ± 7.5 nM 1.13 ± 0.36 μM 41.7 ± 4.7 nM 119 ± 34.1 nM
Fenobam 178 ± 40 nM 2.93 ± 0.48 μM 442 ± 150 nM 807 ± 53.5 nM
AFQ056 37.6 ± 8.9 nM 9.44 ± 3.78 μM 257 ± 27.4 nM 270 ± 73.0 nM
RG7090 1.76 ± 0.88 nM 62.0 ± 17.5 nM 8.97 ± 3.40 nM 80.2 ± 16.8 nM
AZD2066 27.2 ± 9.1 nM 3.56 ± 0.52 μM 96.2 ± 17.8 nM 380 ± 78.0 nM
a

The IC50 values of various mGlu5 NAMs were determined from the inhibition curves in Figure 4 using GraphPad Prism.