Binding of progestins to the glucocorticoid receptor

摘要: A number of physiological and synthetic progestins were tested for their ability to compete with [3H]dexamethasone the binding glucocorticoid receptor human mononuclear leukocytes elicit glucocorticoid-like effects on same cells. As compared reference compound dexamethasone (relative affinity defined as 100%), two potent a pregnane-type structure, megestrol acetate medroxyprogesterone acetate, found display considerable towards (46 42%, respectively). The relative naturally occurring ligand, cortisol, was clearly lower (25%). effective confirmed by direct studies utilizing tritiated derivative this steroid. No evidence existence specific progesterone in obtained judged results competition experiments where receptor-specific ligand [3H]Org 2058 used. Medroxyprogesterone also induced lymphocyte functions. These included inhibition proliferative responses T-cell mitogens concanavalin phytohaemagglutinin an enhanced accumulation immunoglobulin secreting cells pokeweed mitogen-stimulated cultures. progestin effect appears be mediated through radiosensitive (suppressor) subpopulation T lymphocytes. In contrast, related structurally 19-nortestosterone, norethisterone d-norgestrel, virtually devoid nor did they measurably influence vitro demonstrate that certain common clinical use probably possess inherent activity suggest side attributable character (e.g. suppression pituitary-adrenal axis) might expected when these compounds are used pharmacological doses.