17beta-Estradiol is the major pre-menopausal bioactive estrogen and an active metabolite of testosterone. It is produced primarily by the ovary, and to a lesser extent, by the adrenals, testes, and adipose tissue, as well as by the placenta during pregnancy. 17beta-Estradiol binds to estrogen receptors localized to...

AMP-activated protein kinase (AMPK) plays a role in energy metabolism and glucose homeostasis by monitoring the ratio of ATP to AMP. AMPK stimulates glucose uptake in skeletal muscle when activated during muscle contraction and exercise by the phosphorylation of threonine 172 (Thr172) by LKB19 and...

Mifepristone is an antagonist of glucocorticoid, progesterone, and androgen receptors (Kis = 0.1, 0.64, and 0.65 nM, respectively). It is selective for these receptors over the mineralocorticoid receptor (MR), estrogen receptor alpha (ERalpha), and ERbeta (Kis = 640, >200, and >750 nM, respectively). In cell-based...

Numerous analogs of arachidonoyl ethanolamide (AEA) potentiate its biological activity. This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty amide acyl hydrolase (FAAH) within the neurons. VDM11 is an AEA transport inhibitor with essentially no activity on either...