TABLE 2

Potency and maximal response indices for potentiation by mGlu5 receptor PAMs of [3H]IPx accumulations stimulated by an EC20 concentration (50 nM) of the orthosteric agonist quisqualate in astrocytes

pEC50 values are given as −log (molar) values, and maximum potentiation values are given as a fold increase in [3H]IPx accumulation compared with the response stimulated in the presence of 50 nM quisqualate alone. Data are shown as means ± S.E.M. for four to five separate experiments each performed in duplicate. Also shown are equilibrium dissociation constants (pKB) and net cooperativity (αβ) with respect to quisqualate; the efficacy cooperativity (β) is estimated by dividing the overall cooperativity (αβ) by the affinity cooperativity (α; Table 1).

Modulator Curve pEC50Potentiation IncreaseAffinity, pKBCooperativity, αβEfficacy Cooperativity, β
log Mfold
DFB5.38 ± 0.111.45 ± 0.075.452.11.4
CPPHA5.73 ± 0.053.21 ± 0.385.724.7N.D.
CDPPB6.24 ± 0.124.55 ± 0.366.27252.3
ADX472735.54 ± 0.104.71 ± 0.665.52309.4
  • N.D., not determined.