3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
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3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol is a
synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic o ...
,
steroid A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and a ...
al estrogen and a selective
agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
of the ERβ. It was discovered serendipitously and was the lead compound among a series of androsta-3,5-dienes as ERβ ligands. Its
affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Partn ...
( IC50) for the ERβ was found to be 9 nM and it showed 62- and 160-fold binding selectivity for this receptor over the and the ERα, respectively. The EC50 of the compound for the ERβ was found to be 69 nM and its intrinsic activity was 92% (relative to that of estradiol). As such, it is a potent ERβ agonist with high affinity and selectivity.


References

Secondary alcohols Androstanes Selective ERβ agonists Synthetic estrogens {{genito-urinary-drug-stub