Table 2.
Relative Potency/Affinity of some mineralocorticoid receptor (MR) and glucocorticoid receptor (GR) agonists and antagonists.
| Agonists | MR:GR Relative Potency | Notes |
|---|---|---|
| MR Agonist | ||
| aldosterone | 600:1 | |
|
| ||
| fludrocortisone | 12.5:1 | Used clinically as mineralocorticoid |
|
| ||
| GR Agonist | ||
|
| ||
| RU28362 | 1:800 | |
|
| ||
| dexamethasone | 1:25 | Used clinically as glucocorticoid |
|
| ||
| MR/GR Agonist | ||
|
| ||
| Cortisol/hydrocortisone | 5:1 | |
|
| ||
| corticosterone | 5:1 | |
|
| ||
| prednisolone | 1:5 | Used clinically as glucocorticoid |
|
| ||
| Antagonists | MR:GR Relative Affinity | |
|
| ||
| MR Antagonist | ||
|
| ||
| spironolactone | 25:1 | Also blocks androgen receptor and stimulates progesterone receptor |
|
| ||
| eplerenone | >100:1 | Less androgen and progesterone receptor cross reactivity than spironolactone, but also lower MR affinity |
|
| ||
| RU28318 | ? | Less androgen receptor cross reactivity than spironolactone |
|
| ||
| GR Antagonist | ||
|
| ||
| RU486 | 1:200 | Also blocks progesterone receptor; has partial GR agonist effects |