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Liquiritigenin
Liquiritigenin is a flavanone that was isolated from ''Glycyrrhiza uralensis'', and is found in a variety of plants of the Glycyrrhiza genus, including ''Glycyrrhiza glabra'' (licorice). It is an estrogenic compound which acts as a selective agonist of the Estrogen receptor beta, ERβ subtype of the estrogen receptor (ER), though it is also reported to act as an ERα partial agonist at sufficient concentrations. It also has a choleretic effect. Liquiritigenin,NADPH:oxygen oxidoreductase (hydroxylating, aryl migration) is an enzyme that uses liquiritigenin, O2, NADPH and H+ to produce 2,7,4'-trihydroxyisoflavanone, H2O, and NADP+. See also * Menerba * Prinaberel (ERB-041) * Diarylpropionitrile (DPN) * WAY-200070 * PHTPP * (R,R)-Tetrahydrochrysene ((R,R)-THC) * Propylpyrazoletriol (PPT) * Methylpiperidinopyrazole (MPP) References Aromatase inhibitors Phytoestrogens Flavanones Selective ERβ agonists {{aromatic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Menerba
Menerba, also known as Menopause Formula 101 (MF-101), is a botanical drug candidate that acts as a selective estrogen receptor modulator (SERM) which is being studied for its potential to relieve hot flashes associated with menopause. Menerba, an estrogen receptor beta (ERβ) agonist (ERBA), is part of a new class of receptor subtype-selective estrogens, which is selective in transcriptional regulation to one of the two known estrogen receptor (ER) subtypes. Menerba consists of 22 herbs that have been used historically in traditional Chinese medicine. Menerba binds to both ERα and ERβ and with equal affinity (pharmacology), affinity, but does not activate ERα and instead activates only ERβ-mediated gene transcription. Mode of action Menerba has been reported to alleviate menopausal symptoms such as hot flashes, while having no stimulative effects on endometrium or breast tissue. In mouse xenograft models, Menerba produced a different conformation in estrogen receptor alpha ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diarylpropionitrile
Diarylpropionitrile (DPN), also known as 2,3-bis(p-hydroxyphenyl)propionitrile (2,3-BHPPN), is a synthetic, nonsteroidal, and highly selective agonist of ERβ ( IC50 = 15 nM) that is used widely in scientific research to study the function of this receptor. It is 70-fold more selective for ERβ over ERα, and has 100-fold lower affinity for GPER (GPR30) relative to estradiol. DPN produces antidepressant- and anxiolytic-like effects in animals via activation of the endogenous oxytocin system. First reported in 2001, DPN was the first selective ERβ agonist to be discovered, and was followed by prinaberel (ERB-041, WAY-202041), WAY-200070, and 8β-VE2 in 2004, ERB-196 (WAY-202196) in 2005, and certain phytoestrogens like liquiritigenin and nyasol (''cis''-hinokiresinol) since 2007. DPN is a racemic mixture of two enantiomers, (R)-DPN and (S)-DPN. Relative to (R)-DPN, (S)-DPN has between 3- and 7-fold higher affinity for ERβ and appears to have higher intrinsic activity in activat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flavanone
The flavanones, a type of flavonoids, are various aromatic, colorless ketones derived from flavone that often occur in plants as glycosides. List of flavanones * Blumeatin * Butin * Dichamanetin * Eriodictyol * Hesperetin * Hesperidin * Homoeriodictyol * Isosakuranetin * Naringenin * Naringin * Pinocembrin * Poncirin * Sakuranetin * Sakuranin * Sterubin * Pinostrobin Metabolism The enzyme chalcone isomerase uses a chalcone-like compound to produce a flavanone. Flavanone 4-reductase is an enzyme that uses (2''S'')-flavan-4-ol The flavan-4-ols (3-deoxyflavonoids) are flavone-derived Alcohol (chemistry), alcohols and a family of flavonoids. Flavan-4-ols are colorless precursor compounds that polymerize to form red phlobaphene pigments. They can be found in the sorghum. Gl ... and NADP+ to produce (2''S'')-flavanone, NADPH, and H+. Synthesis Numerous methods exist for the enantioselective chemical and biochemical synthesis of flavanones and related compounds. Re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phytoestrogens
A phytoestrogen is a plant-derived xenoestrogen (a type of estrogen produced by organisms other than humans) not generated within the endocrine system, but consumed by eating plants or manufactured foods. Also called a "dietary estrogen", it is a diverse group of naturally occurring nonsteroidal plant compounds that, because of its structural similarity to estradiol (17-β-estradiol), have the ability to cause both estrogenic or antiestrogenic effects. Phytoestrogens are not essential nutrients because their absence from the diet does not cause a disease, nor are they known to participate in any normal biological function. Common foods containing phytoestrogens are soybeans and soy protein concentrate, miso, tempeh, and tofu. Some soy-based infant formulas manufactured with soy protein contain isoflavones. Its name comes from the Greek language, Greek ''phyto'' ("plant") and ''estrogen'', the hormone which gives fertility to female mammals. The word "estrus" (Greek οίστ� ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatase Inhibitors
Aromatase inhibitors (AIs) are a class of medication, drugs used in the treatment of breast cancer in menopause, postmenopausal women and in men, and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer. Aromatase is the enzyme that catalyzes a key aromatization step in the synthesis of estrogen. It converts the Alpha-beta Unsaturated carbonyl compounds, enone ring of androgen precursors such as testosterone, to a phenol, completing the synthesis of estrogen. As such, AIs are estrogen synthesis inhibitors. Because hormone-positive breast and ovarian cancers are dependent on estrogen for growth, AIs are taken to either block the production of estrogen or block the action of estrogen on receptors. Medical uses Cancer In contrast to premenopausal women, in whom most of the estrogen is produced in the ovary, ovaries, in postmeno ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methylpiperidinopyrazole
Methylpiperidinopyrazole (MPP) is a synthetic, nonsteroidal, and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor. It has 200-fold selectivity for ERα over ERβ and 1000-fold selectivity for blocking ERα-mediated gene transcription relative to that of ERβ. See also * Glyceollin * Propylpyrazoletriol (PPT) * Diarylpropionitrile (DPN) * Prinaberel (ERB-041) * Liquiritigenin * Menerba Menerba, also known as Menopause Formula 101 (MF-101), is a botanical drug candidate that acts as a selective estrogen receptor modulator (SERM) which is being studied for its potential to relieve hot flashes associated with menopause. Menerba, an ... * PHTPP * (R,R)-Tetrahydrochrysene ((R,R)-THC) References Antiestrogens 1-Piperidinyl compounds Phenol ethers 4-Hydroxyphenyl compounds Pyrazoles {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Propylpyrazoletriol
Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal agonist of ERα with 400-fold selectivity over ERβ that is used widely in scientific research to study the function of ERα. Though originally thought to be highly selective for ERα, PPT has subsequently been found to also act as an agonist of the GPER (GPR30). See also * ERA-45 * ERA-63 ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidal estrogen and a selective agonist of the ERα that was under development for the treatment of rheumatoid arthritis bu ... * GTx-758 * Methylpiperidinopyrazole (MPP) References GPER agonists Ketones 4-Hydroxyphenyl compounds Pyrazoles Synthetic estrogens {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
(R,R)-Tetrahydrochrysene
(''R'',''R'')-Tetrahydrochrysene ((''R'',''R'')-THC) is a drug used to study the estrogen receptors (ERs) in scientific research. It is an ERβ antagonist and an ERα agonist with 10-fold higher affinity for ERβ relative to ERα. (''R'',''R'')-THC is a silent antagonist of ERβ, and, uniquely relative to other known ERβ antagonists, a passive antagonist of the receptor. (''S'',''S'')-Tetrahydrochrysene ((''S'',''S'')-THC) also binds to the ERs, but in contrast to (''R'',''R'')-THC, (''S'',''S'')-THC is an agonist of both ERα and ERβ and has 20-fold lower affinity for ERβ relative to (''R'',''R'')-THC. See also * Propylpyrazoletriol (PPT) * PHTPP * Methylpiperidinopyrazole (MPP) * Diarylpropionitrile (DPN) * Prinaberel (ERB-041) * Liquiritigenin * Menerba * 2,8-DHHHC * Chrysene Chrysene is a polycyclic aromatic hydrocarbon (PAH) with the molecular formula that consists of four fused benzene rings. It is a natural constituent of coal tar, from which it was first isol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PHTPP
PHTPP is a synthetic, nonsteroidal, and highly selective antagonist of ERβ that is used in scientific research to study the function of this receptor. It possesses 36-fold selectivity for ERβ over ERα, and is a silent antagonist of ERβ. See also * Propylpyrazoletriol (PPT) * Methylpiperidinopyrazole (MPP) * (R,R)-Tetrahydrochrysene ((R,R)-THC) * Diarylpropionitrile (DPN) * Prinaberel (ERB-041) * Liquiritigenin * Menerba * WAY-200070 WAY-200070 is a synthetic compound, synthetic, nonsteroidal, highly binding selectivity, selective agonist of ERβ. It possesses 68-fold selectivity for ERβ over ERα (EC50, EC50 = 2 nM and 155 nM, respectively). WAY-200070 has been found to enh ... References Antiestrogens Trifluoromethyl compounds 4-Hydroxyphenyl compounds Pyrazolopyrimidines {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WAY-200070
WAY-200070 is a synthetic compound, synthetic, nonsteroidal, highly binding selectivity, selective agonist of ERβ. It possesses 68-fold selectivity for ERβ over ERα (EC50, EC50 = 2 nM and 155 nM, respectively). WAY-200070 has been found to enhance Serotonin, serotonergic and dopaminergic neurotransmission in the central nervous system, and produces antidepressant- and anxiolytic-like effects in animals. It has been proposed as a potential novel antidepressant/anxiolytic agent. WAY-200070 has also been found to produce antidiabetic effects in animals, and may also be beneficial for the treatment of certain inflammation, inflammatory conditions. Due to its selectivity for ERβ, WAY-200070 is inactive in various assays of classic estrogen action, such as uterotrophic and osteopenia. Moreover, WAY-200070 does not affect luteinizing hormone or follicle-stimulating hormone or inhibit ovulation, indicating that it does not suppress the hypothalamic-pituitary-gonadal axis, and as ERα ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prinaberel
Prinaberel (International Nonproprietary Name, INN, United States Adopted Name, USAN) (developmental code names ERB-041, WAY-202041) is a synthetic compound, synthetic, nonsteroidal, and highly binding selectivity, selective agonist of the estrogen receptor beta, ERβ isoform, subtype of the estrogen receptor. It is used in scientific research to elucidate the role of the ERβ receptor. Studies have indicated that selective ERβ agonists like prinaberel could be useful in the clinical treatment of a variety of medical conditions including inflammatory bowel disease, rheumatoid arthritis, endometriosis, and sepsis. Accordingly, prinaberel either was or still is under investigation by Wyeth for the treatment of some of these conditions. See also * Diarylpropionitrile * ERB-196 * Erteberel * WAY-200070 * WAY-214156 References External links Prinaberel - AdisInsight Benzoxazoles Fluoroarenes Selective ERβ agonists {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
