Table 1.
AR Binding and Transactivation
| Androgen | Binding to ARLBD | Transactivation in CV-1 Cells |
|
|---|---|---|---|
| IC50 (nM)1 | RBA (%)2 | EC50 (nM)1 | |
| R1881 | 4.4 ± 0.4 (12) | 1003 | 0.39 ± 0.15 (7) |
| T | 27.2 ± 3.1a (4) | 22 | 16.8 ± 6.1a (9) |
| DHT | 21.4 ± 3.4a (14) | 33 | 6.5 ± 2.5a,b (10) |
| DMA | 9.5 ± 1.8ab (5) | 106 | 1.5 ± 0.6b (7) |
| 5α-DHDMA | 5.5 ± 1.1b (4) | 105 | 5.9 ± 2.6 a,b (7) |
| MNT | 5.9 ± 0.6b (6) | 105 | 1.9 ± 0.7a,b (7) |
| 5α-DHMNT | 7.9 ± 1.1a,b (5) | 86 | 5.5 ± 4.1a,b (5) |
| MENT | 9.3 ± 0.5a,b (5) | 72 | 3.1 ± 1.0 a,b (3) |
| 5α-DHMENT | 17.6 ± 0.3a,b (3) | 26 | 2.2 ± 1.9 a,b (4) |
1
Values represent the mean ± SE the number of determinations indicated in parentheses.
2
The relative binding affinity (RBA) % = IC50 R1881/IC50 test compound X 100.
3
The RBA for R1881, the reference standard, is arbitrarily defined as 100%.
a
Means with different letters are significantly different (P<0.05).
b
Means with different letters are significantly different (P<0.05).