Table 3.
Ki (nM) |
Relative affinitya |
||||
---|---|---|---|---|---|
1 h incubation | 4 h incubation | Ratio | 1 h incubation | 4 h incubation | |
Urotensin-II | 0.2±0.0 | 0.3±0.1 | 1.5 | 0.1 | 0.2 |
SB-657510 | 56.9±9.7 | 213.0±71.2 | 3.7 | 0.9 | 3.5 |
Palosuran | 49.8±3.3 | 192.5±57.2 | 3.9 | 9.8 | 37.7 |
Abbreviation: hUT, human urotensin-II receptor.
Relative affinity is expressed as the native human UT Ki relative to the corresponding value obtained in recombinant hUT membrane preparations (see Table 1). All values are expressed as mean±s.e.m. Statistical comparisons were made using an unpaired, two-tailed t-test and no values were determined from 1 h (n=3).