Receptor density and pharmacological profile of human recombinant α1A-, α1B-, and α1A,1B-ARs stably expressed in HEK 293 cells
Parentheses show the density or proportion of each subtype. Competition experiments were done at 4 and 37°C. Data are shown as the mean ± S.E.M. of three to four experiments.
Bmax and pKi | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| α1A | α1B | α1A,1B | |||||||||
| Bmax, fmol/mg protein | 1600 ± 520 | 4650 ± 690 | 5860 ± 790 (1410/4450) | ||||||||
| 4°C | 37°C | 4°C | 37°C | 4°C | 37°C | ||||||
| Prazosin | 9.9 ± 0.1 | 9.7 ± 0.2 | 10.4 ± 0.1 | 10.2 ± 0.1 | 10.2 ± 0.1 | 10.2 ± 0.2 | |||||
| KMD-3213 | 10.4 ± 0.1 | 10.3 ± 0.2 | 7.9 ± 0.1 | 7.6 ± 0.3 | 10.3 ± 0.2 (23%) | 10.2 ± 0.3 (25%) | |||||
| 7.6 ± 0.1 (77%) | 7.8 ± 0.2 (75%) | ||||||||||
| Phenylephrine | 5.7 ± 0.2 | 5.6 ± 0.2 | 5.7 ± 0.1 | 5.5 ± 0.1 | 5.7 ± 0.1 | 5.9 ± 0.1 | |||||
| Methoxamine | 5.5 ± 0.4 | 5.9 ± 0.1 | 4.1 ± 0.1 | 4.0 ± 0.2 | 6.1 ± 0.1 (25%) | 5.9 ± 0.1 (28%) | |||||
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| 3.9 ± 0.2 (75%) | 3.8 ± 0.2 (71%) | |||||
pKi, negative logarithm of the equilibrium dissociation constant.