Table 1.
Competition of agonists versus [3H]-8-OH DPAT binding to membranes of CHO cells expressing the human 5-HT1A receptor
| Ligand | DPAT | 5-OH DPAT | 6-OH DPAT | 7-OH DPAT | 8-OH DPAT | |||||
|---|---|---|---|---|---|---|---|---|---|---|
| enantiomer | R | S | R | S | R | S | R | S | R | S |
| pKi±s.e.m. | 7.94±0.12 | 6.97±0.23 | 6.31±0.10 | 6.65±0.15 | 5.86±0.07 | 5.54±0.06 | 7.21±0.08 | 6.50±0.05 | 9.41±0.07 | 9.27±0.09 |
| (Ki (nM)) | (11.5) | (108) | (492) | (223) | (1371) | (2865) | (62) | (316) | (0.39) | (0.53) |
| n | 3 | 3 | 4 | 4 | 4 | 4 | 4 | 4 | 5 | 5 |
The binding of a series of agonists was determined in competition versus [3H]-8-OH DPAT as described in the Methods section. Competition curves were fitted well by one-binding site models in all cases (P<0.05) and Ki values (pKi mean±s.e.m., n experiments) are recorded.