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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, nonsteroidal, highly selective agonist of ERβ. It possesses 68-fold selectivity for ERβ over ERα ( EC50 = 2 nM and 155 nM, respectively). WAY-200070 has been found to enhance serotonergic and dopaminergic neurotr ... References Antiestrogens Trifluoromethyl compounds Phenols Pyrazolopyrimidines {{pharmacology-stub ... [...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 * 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. ... * (R,R)-Tetrahydrochrysene ((R,R)-THC) References Antiestrogens 1-Piperidinyl compounds Phenol ethers Phenols Pyrazoles {{genito-urinary-drug-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 isola ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen Receptor Beta
Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen. In humans ERβ is encoded by the ''ESR2'' gene. Function ERβ is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17-β-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor α that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Liquiritigenin
Liquiritigenin is a flavanone that was isolated from ''Glycyrrhiza uralensis'', and is found in a variety of plants, including ''Glycyrrhiza glabra'' (licorice). It is an estrogenic compound which acts as a selective agonist of the 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 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 ERΠ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluoromethyl Compounds
The trifluoromethyl group is a functional group that has the formula -CF3. The naming of is group is derived from the methyl group (which has the formula -CH3), by replacing each hydrogen atom by a fluorine atom. Some common examples are trifluoromethane H–, 1,1,1-trifluoroethane –, and hexafluoroacetone –CO–. Compounds with this group are a subclass of the organofluorines. Properties The trifluoromethyl group has a significant electronegativity that is often described as being intermediate between the electronegativities of fluorine and chlorine. For this reason, trifluoromethyl-substituted compounds are often strong acids, such as trifluoromethanesulfonic acid and trifluoroacetic acid. Conversely, the trifluoromethyl group lowers the basicity of compounds like trifluoroethanol. Uses The trifluoromethyl group occurs in certain pharmaceuticals, drugs, and abiotically synthesized natural fluorocarbon based compounds. The medicinal use of the trifloromethyl group dates from ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiestrogens
Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production., Antiestrogens are one of three types of sex hormone antagonists, the others being antiandrogens and antiprogestogens. Antiestrogens are commonly used to stop steroid hormones, estrogen, from binding to the estrogen receptors leading to the decrease of estrogen levels. Decreased levels of estrogen can lead to complications in sexual development. Antiandrogens are sex hormone antagonists which are able to lower the production and the effects that testosterone can have on female bodies. Types and examples Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestran ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WAY-200070
WAY-200070 is a synthetic, nonsteroidal, highly selective agonist of ERβ. It possesses 68-fold selectivity for ERβ over ERα ( EC50 = 2 nM and 155 nM, respectively). WAY-200070 has been found to enhance 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 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 and not ERβ is implicated in breast development, would not be ... [...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, 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 (ERα) from ERβ when compa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prinaberel
Prinaberel (INN, USAN) (developmental code names ERB-041, WAY-202041) is a synthetic, nonsteroidal, and highly selective agonist of the ERβ 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 WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ. It is 100-fold selective for the ERβ over the ERα with an IC50 of 4.2 nM (compare to estradiol with IC50 values of ~3–4 nM for b ... References External links Prinaberel - AdisInsigh ... [...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] |
Synthetic Compound
In chemistry, organic compounds are generally any chemical compounds that contain carbon-hydrogen or carbon-carbon bonds. Due to carbon's ability to catenate (form chains with other carbon atoms), millions of organic compounds are known. The study of the properties, reactions, and syntheses of organic compounds comprise the discipline known as organic chemistry. For historical reasons, a few classes of carbon-containing compounds (e.g., carbonate salts and cyanide salts), along with a few other exceptions (e.g., carbon dioxide, hydrogen cyanide), are not classified as organic compounds and are considered inorganic. Other than those just named, little consensus exists among chemists on precisely which carbon-containing compounds are excluded, making any rigorous definition of an organic compound elusive. Although organic compounds make up only a small percentage of Earth's crust, they are of central importance because all known life is based on organic compounds. Living t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal
A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor modulators Examples include the following: * Estrogens: benzestrol, bifluranol, estrobin (DBE), diethylstilbestrol (stilbestrol), dienestrol, erteberel, fosfestrol, hexestrol (dihydroxystilbestrol), methallenestril, methestrol, methestrol dipropionate, paroxypropione, prinaberel, and triphenylethylene, as well as many xenoestrogens * : acolbifene, afimoxifene, arzoxifene, bazedoxifene, broparestrol, chlorotrianisene, clomifene, clomifenoxide, cyclofenil, droloxifene, enclomifene, endoxifen, ethamoxytriphetol, fispemifene, idoxifene, lasofoxifene, levormeloxifene, miproxifene, nafoxidine, nitromifene, ormeloxifene, ospemifene, panomifene, pipendoxifene, raloxifene, tamoxifen, toremifene, trioxifene, zindoxifene, zuclomifene * An ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
