TABLE 2

Efficacy (τB) of NPS R568 and AC265347 determined in Ca2+i mobilization assays using an interaction paradigm

Data are mean ± S.E.M. and 95% confidence intervals from the indicated number of independent experiments (n).

NPS R568AC265347
LogτB (95% CI) (τB)nLogτB (95% CI) (τB)n
WTND17−0.22 ± 0.09 (−0.45 to −0.08) (0.6)8
F6121.39AND40.12 ± 0.09a (−0.10 to 0.44) (1.3)4
A6151.42VND60.04 ± 0.03 (−0.01 to 0.09) (1.1)4
F6682.56AND4ND4
G670ECL1A−0.25 ± 0.06 (−0.41 to −0.15) (0.6)4−0.15 ± 0.09 (−0.39 to 0.02) (0.7)4
F6843.36AND4ND5
F6883.40AND5ND4
E767ECL2AND30.05 ± 0.03 (−0.02 to 0.12) (1.1)4
A7725.39VND4ND4
F7755.42AND4−0.26 ± 0.07 (−0.48 to 0.14) (0.5)7
L7765.43AND40.19 ± 0.12a (−0.11 to 0.32) (1.5)6
V8176.49AND40.33 ± 0.04a,b (0.26–0.45) (2.1)5
W8186.50AND5ND4
F8216.53AND4ND4
Y8256.57AND4ND4
K831ECL3AND4−0.05 ± 0.03 (−0.10 to 0.00) (0.9)5
V833ECL3AND4ND5
E8377.32DND40.09 ± 0.12 (−0.18 to 0.28) (1.2)4
E8377.32INA7NA5
A8407.35VND4ND7
I8417.36ANA4ND4
A8447.39V−0.22 ± 0.07 (−0.45 to −0.11) (0.6)5−0.12 ± 0.03 (−0.14 to −0.09) (0.8)6
L8487.43AND4−0.17 ± 0.07 (−0.35 to −0.07) (0.7)4
  • CI, confidence interval; NA, negligible PAM activity; ND, not determined due to negligible efficacy.

  • a Significantly different from WT (P < 0.05, one-way ANOVA with Dunnett’s multiple comparisons post-test).

  • b To account for a reduction in cell surface expression caused by V8176.49A compared with the WT CaSR (Leach et al., 2016), logτB was normalized to determine what it would be if this mutant was expressed at the same level as the WT receptor (Gregory et al., 2010).