The agonistic and antagonistic actions of estriol.

Estriol is a short acting estrogen, and as such, displays both agonistic and antagonistic properties, when it is injected in saline solution. These are predictable attributes of any short acting agonist if one considers the basic pharmacology of receptor ligand binding interactions. That is, short acting hormones or drugs occupy receptor sites for protracted time periods and, although they stimulate responses, these are of short duration. However, when estriol is administered in continuous fashion the estrogen receptor is occupied for long periods of time and full estrogenic responses are observed, and there is no antagonism of estradiol action. The purpose of this paper is to review the work that leads to the above conclusion and to discuss our more recent work on the relationship between estrogen receptor binding and the stimulation of type II estrogen binding sites.