GPER agonist
G protein-coupled estrogen receptor (GPER) agonist
- Fast, non-genomic estrogen signaling → vasodilation and neuroprotection
- Membrane-bound; also neuroendocrine and metabolic modulation
- Calcium mobilization, kinase activation — cardioprotection
- Distinct from the slow nuclear ERα/ERβ transcriptional actions
Drugs with this mechanism (7)
- Conjugated estrogens — Estrogen mixture for menopausal symptoms.
- Estradiol — Principal human estrogen; available systemically or locally for menopausal symptoms.
- Estradiol transdermal — Skin-delivered estrogen for menopausal symptoms; avoids first-pass hepatic exposure.
- Estradiol vaginal — Local estrogen for menopausal genitourinary symptoms; little systemic exposure.
- Estriol — Relatively weak estrogen prominent in pregnancy; used vaginally for menopausal symptoms in some countries, but not FDA-approved.
- Estrone — Major circulating estrogen after menopause, formed largely by peripheral aromatization; interconverts with the more potent estradiol.
- Ethinyl estradiol — The synthetic estrogen in most combined oral contraceptives.
Self-check
- Is GPER estrogen signaling genomic or non-genomic?
Fast and non-genomic. - Which intracellular processes accompany GPER-mediated cardioprotection?
Calcium mobilization and kinase activation.
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