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. 2017 May 22;60(12):5072–5085. doi: 10.1021/acs.jmedchem.7b00410

Figure 3.

Figure 3

(A) Ca2+ mobilization assay CRC for 27 in HEK293A cells expressing human mGlu5. (B) Effects of 27 on glutamate CRC in rat cortical astrocytes. (C) Competition radioligand binding CRC with 27 and [3H]-3-methoxy-5-(pyridin-2-ylethynyl)pyridine (39). (D) Saturation binding experiment: increasing concentrations of [3H]-39 in the presence and absence of multiple concentrations of 27. (E) Saturation binding experiment: Scatchard analysis of bound/free versus bound ligand. (F) Effects of the neutral mGlu5 site ligand 5-methyl-6-(phenylethynyl)-pyridine (40) on the functional inhibition of glutamate responses induced by 27.