ERB-041 is a potent, selective ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα)
ERB-041 is a potent, selective estrogen ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα). ERβ plays a minor role in mediating estrogen action in the uterus, the hypothalamus/pituitary, the skeleton, and other classic estrogen target tissues. However, a clear role for ERβ has been established in the ovary, cardiovascular system, and brain as well as in animal models of inflammation including arthritis, endometriosis, inflammatory bowel disease, and sepsis. There is increasing interest in finding ERβ agonists for potential use in a variety of clinical applications without triggering classic estrogenic side effects.
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This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Estrogen receptor beta (ERβ) has been shown to play a therapeutic role in inflammatory bowel disease (IBD). However, the mechanism underlying how ERβ exerts therapeutic effects and its relationship with P2X3 receptors (P2X3R) in rats with inflammation is not known.
It is well known that estrogens and estrogen-like endocrine disruptors can suppress steroidogenic gene expression, attenuate androgen production and decrease differentiation of adult Leydig cell lineage. However, there is no information about the possible link between the potency of Leydig
The Journal of pathology, 251(3), 297-309 (2020-04-26)
Oestrogen receptor β (ERβ) has been suggested to have anti-proliferative and anti-tumour effects in breast and prostate cancer cells, but other studies have indicated its tumour-promoting effects. Understanding the complex effects of this receptor in different contexts requires further study.
Estrogens produce biological effects by interacting with two estrogen receptors, ERalpha and ERbeta. Drugs that selectively target ERalpha or ERbeta might be safer for conditions that have been traditionally treated with non-selective estrogens. Several synthetic and natural ERbeta-selective compounds have
Estrogens are used extensively to treat hot flashes in menopausal women. Some of the beneficial effects of estrogens in hormone therapy on the brain might be due to nongenomic effects in neurons such as the rapid stimulation of calcium oscillations.
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