TABLE 2

Parameter estimates from [3H]NMS off-rate assays Parameters for the inhibition of [3H]NMS dissociation measured at a single time were derived from fitting three assays such as those shown in Fig. 4 to a logistic function. pEC50 is —log of the concentration causing 50% of the maximal effect; according to the allosteric model it corresponds to the log affinity of thiochrome for the [3H]NMS-occupied receptor. Emax is the dissociation rate constant of [3H]NMS, expressed as a percentage of control, in the presence of a saturating concentration of thiochrome. Predicted indicates the pEC50 value predicted by multiplying the mean estimates of affinity and the cooperativity with [3H]NMS from the equilibrium assays summarized in Table 1.

Subtype pEC50 Slope Emax Predicted
%
M1 3.40 ± 0.04 1.7 ± 0.1 0.1 ± 0.1 3.94
M2 3.52 ± 0.06 1.6 ± 0.1 1.7 ± 1.7 3.87
M3 3.17 ± 0.06 1.7 ± 0.1 0.0 ± 0.0 4.23
M4 3.59 ± 0.03 1.5 ± 0.1 0.6 ± 0.6 3.77
M5 2.81 ± 0.17 1.3 ± 0.3 15 ± 15