Effects of change in ligand structure on binding affinity and functional potency at wild-type and S5.43(239)A mutant h5-HT2A receptors
Data are represented as –Δ Δ G° or Δ pEC50 values based on data from Tables 1 and 2. Negative values indicate a loss in binding affinity or functional potency as a result of the change in ligand structure. Values near 0 indicate the receptor is insensitive to the change of ligand structure being compared. Except where indicated (†), all values for –Δ Δ G° or Δ pEC50 generated P < 0.05 from unpaired two-tailed Student's t tests between ligands at the particular receptor compared (column heading).
Drug | -Δ Δ Go | Δ pEC50 | ||||
|---|---|---|---|---|---|---|
| WT h5-HT2A | S5.43(239)A | WT h5-HT2A | S5.43(239)A | |||
| DOM vs. 2-Et-DOM | -1.6 | -1.4 | -1.2 | -0.7 | ||
| DOM vs. 5-Et-DOM | -0.8 | 0.2† | -1.4 | 0.0† | ||
| DOM vs. 5-H-DOM | -2.0 | -1.2 | -2.3 | -0.6 | ||
↵† P > 0.05