Drug | 5-HT2A | S239A | F240A | F243A | F244A | |
---|---|---|---|---|---|---|
K d(nM) | Ketanserin | 1.7 ± 0.29 | 0.62 ± 0.21 | 0.58 ± 0.09 | 5.3 ± 2.0 | |
B max (fmol/mg protein) | 1803 ± 143 | 1089 ± 125 | 1658 ± 85 | 2367 ± 583 | ||
K d (nM) | NMSP | 0.78 ± 0.17 | 6.0 ± 1.7 | |||
B max (fmol/mg protein) | 713 ± 57 | 574 ± 111 |
Data represent means ± S.E. for three separate experiments of mean K d (nM) and B max (fmol/mg protein). For the F243A mutant, [3H]NMSP was used as the radioligand because of the low affinity of ketanserin for F243A. For all other mutants, [3H]ketanserin was used. In a typical experiment, 90% of total binding was specific, and ≤10% of the total radioligand was bound.