Table 4: Comparison of mGlu₅ NAM functional affinity estimates (pK_B) across different measures of receptor activity in primary mouse cortical neurons in the presence and absence of 30 µM CPCCOEt.

Data represent mean ± SEM of indicated number (n) of independent experiments performed in duplicate.

	With CPCCOEt						no CPCCOEt
	iCa2+ (1min)	n	iCa2+ (30min)	n	IP1 accumulation	n	iCa2+ (1min)	n	iCa2+ (30min)	n	IP1 accumulation	n
MPEP	7.61 ±0.20a	6	7.61 ±0.15	5	7.69 ±0.19	11	7.46 ±0.16a	5	7.59 ±0.17	7	7.42 ±0.22	10
fenobam	6.62 ±0.23	4	7.10 ±0.17	4	6.63±0.28	9	6.85 ±0.18	4	7.20 ±0.17	6	6.51 ±0.24	7
VU0409106	6.63 ±0.20	6	7.35 ±0.15	5	6.32 ±0.26b	10	7.08 ±0.17	4	7.28 ±0.18	6	6.68 ±0.24	8
VU0366248	5.99 ±0.35a	7	6.04 ±0.33	5	n.r.	5	5.91 ±0.62a	5	6.86 ±0.29	5	n.r.	5
VU0366058	6.43 ±0.45	6	6.55 ±0.14	6	6.36 ±0.24	10	7.00 ±0.50	6	6.94 ±0.17	6	6.24 ±0.24	8
M-5MPEP	6.47 ±0.30	6	5.64 ±0.25	8	6.24 ±0.39	10	6.93 ±0.48	8	5.98 ±0.29	5	5.94 ±0.31	11
dipraglurant	8.03 ±0.23b	5	7.39 ±0.15	5	6.94 ±0.20c	9	7.16±0.16a	5	7.28 ±0.17	6	6.88 ±0.12	7
MTEP	8.06 ±0.22	5	7.09 ±0.16	4	6.89 ±0.24c	8	7.11±0.28a	5	6.55 ±0.18a,b	6	6.90 ±0.28	8

^aDenotes p<0.05, One-way ANOVA, Sidak’s multiple comparisons test, compared to pK_B estimate derived from modulation of DHPG mediated iCa²⁺ mobilization in HEK293A-rat mGlu₅-low cells under comparable assay paradigm (see Table 2).

^bDenotes p<0.05, One-way ANOVA, Sidak’s multiple comparisons test, compared to binding estimate

^cDenotes p<0.05, One-way ANOVA, Sidak’s multiple comparisons test, compared with pK_B estimate derived from iCa²⁺ mobilization assays using a 1min paradigm

n.r. no modulatory response was evident.