Table 2.
Relative changes in agonist potencies, forward (kon) and reverse (koff) rate constants and calculated kinetic potencies at the S1935.42A mutant, as compared to WT D2R.
Agonist | Potency | Relative Efficacy | koff | kon |
---|---|---|---|---|
DA | ↓↓↓ | − | − | ↓↓↓ |
p-tyramine | ↑ | ↑ | − | ↑ |
(S)-5-OH-DPAT | ↓↓ | − | ↑ | ↓↓ |
(R)-5-OH-DPAT | ↑ | ↑↑ | ↑ | ↑ |
↑↑, strong increase; ↑, weak increase; ↓↓↓, very strong decrease; ↓↓, strong decrease.