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ERB-041
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 - AdisInsight ... [...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] |
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] |
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] |
Endometriosis
Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, fallopian tubes, and tissue around the uterus and ovaries; in rare cases it may also occur in other parts of the body. Some symptoms include pelvic pain, heavy periods, pain with bowel movements, and infertility. Nearly half of those affected have chronic pelvic pain, while in 70% pain occurs during menstruation. Pain during sexual intercourse is also common. Infertility occurs in up to half of affected individuals. About 25% of individuals have no symptoms and 85% of those seen with infertility in a tertiary center have no pain. Endometriosis can have both social and psychological effects. The cause is not entirely clear. Risk factors include having a family history of the condition. The areas of endometriosis bleed each month (menstrua ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzoxazoles
Benzoxazole is an aromatic organic compound with a molecular formula C7H5NO, a benzene-fused oxazole ring structure, and an odor similar to pyridine. Although benzoxazole itself is of little practical value, many derivatives of benzoxazoles are commercially important. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization. Occurrence and applications It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen and tafamidis. Benzoxazole derivatives are also of interest for optical brighteners in laundry detergents.E. Smulders, E. Sung "Laundry Detergents, 2. Ingredients and Products" in ''Ullmann's Encyclopedia of Industrial Chemistry'', Wiley-VCH, Weinheim, 2012. Benzoxazoles belong to the group of well-known antifungal agents with an ... [...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] |
Erteberel
Erteberel (, ; former developmental code name LY-500307; also known as selective estrogen receptor beta agonist-1 or SERBA-1) is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and is under development by Eli Lilly for the treatment of schizophrenia. It is specifically under investigation for the treatment of negative symptoms and cognitive impairment associated with the condition. As of 2015, it is in phase II clinical trials for this indication in the United States. Erteberel was also under investigation for the treatment of benign prostatic hyperplasia and reached phase II clinical studies for this use but failed to improve symptoms in men with the condition and development for this indication was discontinued. The drug has also been proposed as a potential novel treatment for glioblastoma. Erteberel has 14-fold binding selectivity for the ERβ over the ERα (Ki = 0.19 nM versus 2.68 nM, respectively). However, it shows 32-fold functional s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
Wyeth
Wyeth, LLC was an American pharmaceutical company. The company was founded in Philadelphia, Pennsylvania, in 1860 as ''John Wyeth and Brother''. It was later known, in the early 1930s, as American Home Products, before being renamed to Wyeth in 2002. Its headquarters moved to Collegeville, Pennsylvania and Madison, New Jersey, before they were consolidated with Pfizer's in New York City after the 2009 merger. Most of Wyeth's pharmaceutical assets were acquired by Pfizer in 2009, while its infant and maternal nutrition business was acquired by Nestlé in 2012. Wyeth manufactured over-the-counter drugs (OTCs) Robitussin and the analgesic Advil (ibuprofen) as well as prescription drugs Premarin and Effexor. History 1860–1899 In 1860, pharmacists John (1834–1907) and Frank Wyeth opened a drugstore with a small research lab on Walnut Street in Philadelphia. In 1862, on the suggestion of doctors, they began to manufacture large quantities of commonly ordered medicines ... [...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] |
Inflammatory Bowel Disease
Inflammatory bowel disease (IBD) is a group of inflammation, inflammatory conditions of the colon (anatomy), colon and small intestine, Crohn's disease and ulcerative colitis being the principal types. Crohn's disease affects the small intestine and large intestine, as well as the mouth, esophagus, stomach and the anus, whereas ulcerative colitis primarily affects the colon and the rectum. IBD also occurs in dogs and is thought to arise from a combination of host genetics, intestinal microenvironment, environmental components and the immune system. There is an ongoing discussion, however, that the term "chronic enteropathy" might be better to use than "inflammatory bowel disease" in dogs because it differs from IBD in humans in how the dogs respond to treatment. For example, many dogs respond to only dietary changes compared to humans with IBD, who often need Immunosuppression, immunosuppressive treatment. Some dogs may also need immunosuppressant or antibiotic treatment when dieta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
