pentolame

Pentolame is a synthetic 17β-aminoestrogen and an analog of 17β-estradiol (E2). It is being investigated as a potential therapeutic candidate for hormone replacement therapy (HRT) in menopausal women. Pentolame acts as a ligand for the G-protein-coupled receptor for estrogen (GPER1), a transmembrane receptor involved in the progression of various neoplasms. Unlike estradiol and its analog prolame, pentolame has demonstrated a lack of proliferative effects on breast (MCF-7) and cervical (SIHA) cancer cell lines in preclinical studies. Additionally, it has been shown to reduce the phosphorylation of the c-fos oncoprotein in cervical cancer cells. This pharmacological profile suggests that pentolame may provide the benefits of estrogen replacement without the associated risk of inducing the proliferation of certain estrogen-dependent cancer cells.

Other names

N-pentyl-1,3,5(10)-estratrien-3-ol-17β-amine17β-aminoestrogen