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ERB-196
ERB-196, also known as WAY-202196, is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ. It possesses 78-fold selectivity for the ERβ over the ERα. The drug was under development by Wyeth for the treatment of inflammation and sepsis starting in 2004 but development was discontinued by 2011. See also * 8β-VE2 * Diarylpropionitrile * FERb 033 * Prinaberel * WAY-166818 * 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 bot ... References External links ERB-196 - AdisInsight Phenols Fluoroarenes Naphthalenes Nitriles Selective ERβ agonists Synthetic estrogens {{genito-urinary-drug-stub ... [...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] |
8β-VE2
8β-VE2, or 8β-vinylestradiol, also known as 8β-vinylestra-1,3,5(10)-triene-3β,17β-diol, is a synthetic estrogen featuring an estradiol core. It is a highly potent and selective agonist of the ERβ that is used in scientific research to study the function of the ERβ. It has 190-fold higher potency in transactivation assays of the ERβ relative to the ERα and 93- (rat) and 180-fold (human) preference in binding affinity for the ERβ over the ERα. In rodents, 8β-VE2 stimulates follicular growth and to a comparable extent as estradiol, whereas the highly ERα-selective agonist 16α-LE2 has no effect on ovarian follicle development, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles. In contrast, 16α-LE2 stimulates uterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the uterus. Research has determined through experimental rodent studies with e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 both the ERα and ERβ). The drug is less selective for the ERβ than is prinaberel (ERB-041, WAY-202041), another selective ERβ agonist, but is more potent in comparison. WAY-214156 may produce anti-inflammatory effects via the ERβ and has been proposed as a potential treatment for inflammatory conditions such as rheumatoid arthritis. See also * 8β-VE2 * 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 o ... * ERB-196 * FERb 033 * WAY-166818 * WAY-200070 References Phenols Nitriles Selective ERβ agonists ... [...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] |
WAY-166818
WAY-166818 is a synthetic, nonsteroidal estrogen related to WAY-200070 which is used in scientific research. It acts as a highly selective full agonist of the ERβ, with 57- and 164-fold selectivity for the ERβ over the ERα in the rat and mouse, respectively. At the human ERβ and ERα, WAY-166818 has IC50 values of 29 nM and 1227 nM (25-fold difference), respectively. The compound has been verified to cross the blood-brain-barrier in rodents. See also * 8β-VE2 * Diarylpropionitrile * ERB-196 * FERb 033 * Menerba * Prinaberel * 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 Alcohols Benzoxazoles Phenols Selective ERβ agonists Synthetic estrogens {{genito-urinary-drug-stub ... [...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] |
FERb 033
FERb 033 is a synthetic, nonsteroidal estrogen that was synthesized in 2009 and is used in scientific research. It is a potent and selective ERβ agonist (Ki = 7.1 nM, EC50 = 4.8 nM), with 62-fold selectivity for the ERβ over the ERα. See also * 8β-VE2 * Diarylpropionitrile * ERB-196 * Erteberel * Prinaberel * WAY-166818 * 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 Chloroarenes Fluoroarenes Aldoximes Selective ERβ agonists Synthetic estrogens Phenols Biphenyls {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal Estrogen
A nonsteroidal estrogen is an estrogen with a nonsteroidal chemical structure. The most well-known example is the stilbestrol estrogen diethylstilbestrol (DES). Although nonsteroidal estrogens formerly had an important place in medicine, they have gradually fallen out of favor following the discovery of toxicities associated with high-dose DES starting in the early 1970s, and are now almost never used. On the other hand, virtually all selective estrogen receptor modulators (SERMs) are nonsteroidal, with triphenylethylenes like tamoxifen and clomifene having been derived from DES, and these drugs remain widely used in medicine for the treatment of breast cancer among other indications. In addition to pharmaceutical drugs, many xenoestrogens, including phytoestrogens, mycoestrogens, and synthetic endocrine disruptors like bisphenol A, are nonsteroidal substances with estrogenic activity. Pharmacology Nonsteroidal estrogens act as agonists of the estrogen receptors, ERα and ERβ. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective ERβ Agonists
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ERβ
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] |
Sepsis
Sepsis, formerly known as septicemia (septicaemia in British English) or blood poisoning, is a life-threatening condition that arises when the body's response to infection causes injury to its own tissues and organs. This initial stage is followed by suppression of the immune system. Common signs and symptoms include fever, tachycardia, increased heart rate, hyperventilation, increased breathing rate, and mental confusion, confusion. There may also be symptoms related to a specific infection, such as a cough with pneumonia, or dysuria, painful urination with a pyelonephritis, kidney infection. The very young, old, and people with a immunodeficiency, weakened immune system may have no symptoms of a specific infection, and the hypothermia, body temperature may be low or normal instead of having a fever. Severe sepsis causes organ dysfunction, poor organ function or blood flow. The presence of Hypotension, low blood pressure, high blood Lactic acid, lactate, or Oliguria, low urine o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inflammation
Inflammation (from la, wikt:en:inflammatio#Latin, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or Irritation, irritants, and is a protective response involving immune cells, blood vessels, and molecular mediators. The function of inflammation is to eliminate the initial cause of cell injury, clear out necrotic cells and tissues damaged from the original insult and the inflammatory process, and initiate tissue repair. The five cardinal signs are heat, pain, redness, swelling, and Functio laesa, loss of function (Latin ''calor'', ''dolor'', ''rubor'', ''tumor'', and ''functio laesa''). Inflammation is a generic response, and therefore it is considered as a mechanism of innate immune system, innate immunity, as compared to adaptive immune system, adaptive immunity, which is specific for each pathogen. Too little inflammation could lead to progressive tissue destruction by the harmful stimulus (e.g. b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
