Antidepressants do not modulate estrogen receptor alpha-mediated gene expression.
The estrogen receptor alpha has been shown to be activated both in a ligand-dependent and in a ligand independent fashion. We investigated whether antidepressants may directly activate the estrogen receptor alpha or enhance ligand-dependent or ligand-independent activation of the estrogen receptor alpha. Whereas both ligand-dependent and ligand-independent activation of the estrogen receptor alpha could be demonstrated in transient transfection studies, antidepressants neither directly activated the estrogen receptor alpha nor did they enhance ligand-dependent or ligand-independent activation. Thus, there are differences between the glucocorticoid receptor and the estrogen receptor alpha with regard to ligand-independent activation and action of antidepressants.
Hermann
B
B
Max-Planck-Institute of Psychiatry, Munich, Federal Republic of Germany.
Vollmer
I
I
Holsboer
F
F
Rupprecht
R
R
D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology; D002460:Cell Line; D003891:Desipramine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000494:pharmacology; D047628:Estrogen Receptor alpha; D005786:Gene Expression Regulation / Q000187:drug effects* / Q000502:physiology*; D017930:Genes, Reporter / Q000187:drug effects; D000882:Haplorhini; D006801:Humans; D007099:Imipramine / Q000494:pharmacology; D051381:Rats; D011960:Receptors, Estrogen / Q000235:genetics* / Q000502:physiology; D014407:Tumor Cells, Cultured
D000928:Antidepressive Agents; D000929:Antidepressive Agents, Tricyclic; D047628:Estrogen Receptor alpha; D011960:Receptors, Estrogen; D004958:Estradiol; D007099:Imipramine; D003891:Desipramine