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SKF-82,958
SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/ D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal acti .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Synthetic estrogens GSK plc brands D1-receptor agonists D5 receptor agonists Phenols Chloroarenes Allyl compounds {{gastrointestinal-drug-st ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SKF-81,297
SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/ D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self-administration in animals. This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958, but not with certain other D1 full agonists such as A-77,636, reflecting functional selectivity Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a referen ... of D1 activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers. References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Phenols D1-receptor agonists D5 receptor agonists Chloroarenes {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
6-Br-APB
6-Br-APB is a synthetic compound that acts as a selective D1 agonist, with the (''R'')-enantiomer being a potent full agonist, while the (''S'') enantiomer retains its D1 selectivity but is a weak partial agonist. (''R'')-6-Br-APB and similar D1-selective full agonists like SKF-81,297 and SKF-82,958 produce characteristic anorectic effects, stereotyped behaviour and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine Amphetamine (contracted from alpha- methylphenethylamine) is a strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. It is also commonly used .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Dopamine agonists Bromoarenes Allylamines Benzazepanes {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ERα
Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor (mainly found as a chromatin-binding protein) that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ''ESR1'' (EStrogen Receptor 1). Structure The estrogen receptor (ER) is a ligand-activated transcription factor composed of several domains important for hormone binding, DNA binding, and activation of transcription. Alternative splicing results in several ESR1 mRNA transcripts, which differ primarily in their 5-prime untranslated regions. The translated receptors show less variability. Ligands Agonists Non-selective * Endogenous estrogens (e.g., estradiol, estrone, estriol, estetrol) * Natural estrogens (e.g., conjugated equine estrogens) * Synthetic estrogens (e.g., ethinylestradiol, diethylstilbestrol) Selective Agonists of ERα selective over ERβ include: * Propylp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Synthesis
As a topic of chemistry, chemical synthesis (or combination) is the artificial execution of chemical reactions to obtain one or several products. This occurs by physical and chemical manipulations usually involving one or more reactions. In modern laboratory uses, the process is reproducible and reliable. A chemical synthesis involves one or more compounds (known as '' reagents'' or ''reactants'') that will experience a transformation when subjected to certain conditions. Various reaction types can be applied to formulate a desired product. This requires mixing the compounds in a reaction vessel, such as a chemical reactor or a simple round-bottom flask. Many reactions require some form of processing (" work-up") or purification procedure to isolate the final product. The amount produced by chemical synthesis is known as the ''reaction yield''. Typically, yields are expressed as a mass in grams (in a laboratory setting) or as a percentage of the total theoretical quantity that ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amphetamine
Amphetamine (contracted from alpha- methylphenethylamine) is a strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. It is also commonly used as a recreational drug. Amphetamine was discovered in 1887 and exists as two enantiomers: levoamphetamine and dextroamphetamine. ''Amphetamine'' properly refers to a specific chemical, the racemic free base, which is equal parts of the two enantiomers in their pure amine forms. The term is frequently used informally to refer to any combination of the enantiomers, or to either of them alone. Historically, it has been used to treat nasal congestion and depression. Amphetamine is also used as an athletic performance enhancer and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. It is a prescription drug in many countries, and unauthorized possession and distribution of amphetamine are often tightly controlled due to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D5 Receptor Agonists
D5 or D05 may refer to: Arts and fiction * ''Dedication 5'', a 2013 mixtape by American rapper Lil Wayne * D5 class Klingon starships, in the ''Star Trek'' science fiction series * Dimension Delete and Deadly Destruction Day, featured in ''Digimon Xros Wars'' Other uses * Digital 5, a network of leading digital governments * D5 HD, a professional digital video format * Demand 5, a video on demand website * The fifth D: All Things Digital, conference * Nikon D5, a 20.9 megapixel DSLR camera * Trident D5 ballistic missile * Volvo D5 engine, an engine family made by Volvo Cars Transport, aviation and logistics * Citroën D5 * Albatros D.V, a German World War I fighter plane * Identification symbol for ''Nachtjagdgeschwader'' 3, a Luftwaffe night fighter-wing of World War II * Dauair (IATA code D5) * Dublin 5, an Irish postal district * Land Rover D5 - Discovery 5 Roads * D5 motorway (Czech Republic) * D5 road (Croatia), a state road * Detour for the M5 South Western Mo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK Plc Brands , a rendering pipeline
{{disambiguation ...
GSK may refer to: * Galatasaray S.K., a Turkish sports club based in Istanbul * Glycogen synthase kinase * Golden State Killer, a California serial rapist and murderer * GSK plc, formerly GlaxoSmithKline, a multinational pharmaceutical corporation * GTK Scene Graph Kit GTK Scene Graph Kit (GSK) is the rendering and scene graph API for GTK introduced with version 3.90. GSK lies between the graphical control elements (widgets) and the rendering. Like GDK, GSK is part of GTK and licensed under the GNU Lesser Ge ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic Estrogens
Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic organic compounds synthetic chemical compounds based on carbon (organic compounds). * Synthetic peptide * Synthetic biology * Synthetic elements, chemical elements that are not naturally found on Earth and therefore have to be created in experiments Industry * Synthetic fuel * Synthetic oil * Synthetic marijuana * Synthetic diamond * Synthetic fibers, cloth or other material made from other substances than natural (animal, plant) materials Other * Synthetic position, a concept in finance * Synthetic-aperture radar, a type or radar * Analytic–synthetic distinction, in philosophy * Synthetic language in linguistics, inflected or agglutinative languages * Synthetic intelligence a term emphasizing that true intelligence expressed by comput ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen
Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal activity: estrone (E1), estradiol (E2), and estriol (E3). Estradiol, an estrane, is the most potent and prevalent. Another estrogen called estetrol (E4) is produced only during pregnancy. Estrogens are synthesized in all vertebrates and some insects. Their presence in both vertebrates and insects suggests that estrogenic sex hormones have an ancient evolutionary history. Quantitatively, estrogens circulate at lower levels than androgens in both men and women. While estrogen levels are significantly lower in males than in females, estrogens nevertheless have important physiological roles in males. Like all steroid hormones, estrogens readily diffuse across the cell membrane. Once inside the cell, they bind to and activate estrogen receptors (E ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
