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. 2014 Dec 1;172(1):185–200. doi: 10.1111/bph.12937

Table 2.

Pharmacological parameters that govern calcimimetic agonism at the CaS receptor

Ca2+i mobilization IP1 accumulation
pKB ± SEM (n) LogτB ± SEM (τB) pKB ± SEM (n) LogτB ± SEM (τB)
R,R-Calcimimetic B 6.77 ± 0.23 (3) −0.27 ± 0.04 (0.54) 6.48 ± 0.28 (3) −0.16 ± 0.06 (0.69)
S,R-Calcimimetic B 5.44 ± 0.29 (3) −0.10 ± 0.10 (0.79) 5.89 ± 0.26 (3) −0.06 ± 0.07 (0.87)
nor-calcimimetic B 6.44 ± 0.14 (3) −0.10 ± 0.03 (0.79) 5.61 ± 0.29 (3) −0.008 ± 0.09 (0.98)
AC-265347 5.94 ± 0.14 (3) −0.02 ± 0.14 (0.95) 6.04 ± 0.18 (3) 0.08 ± 0.05 (1.1)

Agonist concentration–response curves were fitted to an operational model of agonism (Equation 2013b) (Black and Leff, 1983) to quantify the equilibrium dissociation constant (pKB) of the calcimimetics and their operational measure of agonism (τB).