Table 2.
LSD Dissociation and association rates at wild-type and mutant 5-HT2AR and 5-HT2BR.
Receptor | BMAX ± SEM fmol/mg protein |
Residence Time, min (koff ± SEM) min−1 |
kon ± SEM, M−1 min−1 | Kd, nM (pKd ± SEM) |
---|---|---|---|---|
5-HT2AR wild-type | 2180 ± 350 | 221 (0.005 ± 0.001) | 1.58×107 ± 4.06×106 | 0.33 (9.48 ± 0.11) |
5-HT2aR L229AEL2 | 1650 ± 520 | 50 (0.020 ± 0.003) | 3.34×107 ± 6.20×106 | 0.81 (9.22 ± 0.25) |
5-HT2BR wild-type | 3010 ± 614 | 46 (0.022 ± 0.004) | 2.59×107 ± 3.04×106 | 0.91 (9.08 ± 0.09) |
5-HT2bR L209AEL2 | 3628 ± 598 | 4 (0.236 ± 0.033) | 4.20×107 ± 5.36×106 | 2.31 (8.63 ± 0.08) |
Data were acquired by association and dissociation kinetic experiments conducted in parallel at 37°C using [3H]LSD (concentration range 0.2–5.0 nM). Estimates of koff, kon, and Kd were obtained from three independent experiments performed in duplicate. Residence time was calculated as 1/koff.