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Deudomperidone
Deudomperidone (developmental code name CIN-102; also known as deuterated domperidone) is a dopamine antagonist medication which is under development in the United States for the treatment of gastroparesis. It acts as a selective dopamine D2 and D3 receptor antagonist and has peripheral selectivity. Deudomperidone is a deuterated form of domperidone, and it is suggested that deudomperidone may have improved efficacy, tolerability, and pharmacokinetics compared to domperidone. As of January 2022, deudomperidone is in phase 2 clinical trials for the treatment of gastroparesis. See also * Metopimazine Metopimazine (, , ), sold under the brand names Nortrip, Vogalen, and Vogalene, is an antiemetic of the phenothiazine group which is used to treat nausea and vomiting. It is marketed in Europe, Canada, and South America. As of August 2020, metopi ... * Trazpiroben References External links Deudomperidone - AdisInsight Antiemetics Antigonadotropins Benzimidazoles Chlor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Domperidone
Domperidone, sold under the brand name Motilium among others, is a dopamine antagonist medication which is used to treat nausea and vomiting and certain gastrointestinal problems like gastroparesis (delayed gastric emptying). It raises the level of prolactin in the human body and is used to induce and promote breast milk production. It may be taken by mouth or rectally. Side effects of domperidone include headache, dry mouth, abdominal cramps, diarrhea, and elevated prolactin levels. Secondary to increased prolactin levels, breast changes, milk outflow, menstrual irregularities, and hypogonadism can occur. Domperidone may also cause QT prolongation and has rarely been associated with serious cardiac complications such as sudden cardiac death. However, the risks are small and occur more with high doses. Domperidone acts as a peripherally selective antagonist of the dopamine D2 and D3 receptors. Due to its low entry into the brain, the side effects of do ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Antagonist
A dopamine antagonist, also known as an anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors by receptor antagonism. Most antipsychotics are dopamine antagonists, and as such they have found use in treating schizophrenia, bipolar disorder, and stimulant psychosis. Several other dopamine antagonists are antiemetics used in the treatment of nausea and vomiting. Receptor pharmacology Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. The D1-like class of dopamine receptors is coupled to Gαs/olf and stimulates adenylate cyclase production, whereas the D2-like class is coupled to Gαi/o and thus inhibits adenylate cyclase production. D1-like receptors: D1 and D5 D1-like receptors – D1 and D5 are always found post-synaptically. The genes coding these receptors lack introns, so there are no splice variants. D1 receptors * D1 receptors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metopimazine
Metopimazine (, , ), sold under the brand names Nortrip, Vogalen, and Vogalene, is an antiemetic of the phenothiazine group which is used to treat nausea and vomiting. It is marketed in Europe, Canada, and South America. As of August 2020, metopimazine has been repurposed and is additionally under development for use in the United States for the treatment of gastroparesis. Metopimazine has antidopaminergic, antihistamine, and anticholinergic activity. However, it has also been described as a highly potent and selective dopamine D2 and D3 receptor antagonist. The D2 receptor antagonism of metopimazine is thought to underlie its antiemetic and gastroprokinetic effects. It is said to not readily cross the blood–brain barrier and hence to have peripheral selectivity, in contrast to metoclopramide but similarly to domperidone. Unlike domperidone however, metopimazine shows no hERG inhibition and hence is expected to have a more favorable cardiovascular profile. In contrast to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, and typical of amines. The name comes from the genus name '' Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripherally Selective Drugs
Periphery or peripheral may refer to: Music *Periphery (band), American progressive metal band * ''Periphery'' (album), released in 2010 by Periphery * "Periphery", a song from Fiona Apple's album '' The Idler Wheel...'' Gaming and entertainment *Periphery, a group of political entities in BattleTech, a wargaming franchise *'' The Peripheral'', a 2014 novel by William Gibson **'' The Peripheral'', a streaming series based on Gibson's novel Tech and math * Peripheral, an external device attached to a computer * Peripheral, an alternate mathematical term for boundary parallel in manifold theory *Peripheral cycle, a mathematical term in graph theory Political *Periphery countries, the least developed countries in world systems theory * Periphery (France), statistical area designating a commuter belt around an urban unit * Peripheries of Greece or ''administrative regions of Greece'' (Greek: , '), the country's first-level administrative divisions ** Peripheral units of Gr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Motility Stimulants
Motility is the ability of an organism to move independently, using metabolic energy. Definitions Motility, the ability of an organism to move independently, using metabolic energy, can be contrasted with sessility, the state of organisms that do not possess a means of self-locomotion and are normally immobile. Motility differs from mobility, the ability of an object to be moved. The term vagility encompasses both motility and mobility; sessile organisms including plants and fungi often have vagile parts such as fruits, seeds, or spores which may be dispersed by other agents such as wind, water, or other organisms. Motility is genetically determined, but may be affected by environmental factors such as toxins. The nervous system and musculoskeletal system provide the majority of mammalian motility. In addition to animal locomotion, most animals are motile, though some are vagile, described as having passive locomotion. Many bacteria and other microorganisms, and multicell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deuterated Compounds
Isotopic labeling (or isotopic labelling) is a technique used to track the passage of an isotope (an atom with a detectable variation in neutron count) through a reaction, metabolic pathway, or cell. The reactant is 'labeled' by replacing specific atoms by their isotope. The reactant is then allowed to undergo the reaction. The position of the isotopes in the products is measured to determine the sequence the isotopic atom followed in the reaction or the cell's metabolic pathway. The nuclides used in isotopic labeling may be stable nuclides or radionuclides. In the latter case, the labeling is called radiolabeling. In isotopic labeling, there are multiple ways to detect the presence of labeling isotopes; through their mass, vibrational mode, or radioactive decay. Mass spectrometry detects the difference in an isotope's mass, while infrared spectroscopy detects the difference in the isotope's vibrational modes. Nuclear magnetic resonance detects atoms with different gyromagnetic rati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D3 Antagonists
D3, D03, D.III, D III or D-3 may refer to: Transportation Roads * London Buses route D3, a Transport for London contracted bus route * D3 motorway (Czech Republic), a motorway in the Czech Republic * D3 road (Croatia), a state road in Croatia * D3 motorway (Slovakia), a motorway in northern Slovakia Aircraft * Albatros D.III, a 1916 German biplane fighter aircraft * Dewoitine D.3, a Dewoitine aircraft * Dunne D.3, a British Dunne aircraft * Fokker D.III, a 1916 German single-seat fighter aircraft * Mercedes D.III, a 1914 German 6-cylinder, liquid-cooled inline aircraft engine * Phönix D.III, a variant of the Austro-Hungarian First World War Phönix D.I biplane fighter * Pfalz D.III, a 1917 German fighter aircraft * Schütte-Lanz D.III, a 1918 German fighter aircraft prototype * Siemens-Schuckert D.III, a 1917 German prototype single-seat fighter aircraft Automobiles * Ford D3 platform, a full-size car automobile platform *Peugeot D3, a panel van manufactured from 1950 to 1955 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D2 Antagonists
D, or d, is the fourth letter in the Latin alphabet, used in the modern English alphabet, the alphabets of other western European languages and others worldwide. Its name in English is ''dee'' (pronounced ), plural ''dees''. History The Semitic letter Dāleth may have developed from the logogram for a fish or a door. There are many different Egyptian hieroglyphs that might have inspired this. In Semitic, Ancient Greek and Latin, the letter represented ; in the Etruscan alphabet the letter was archaic, but still retained (see letter B). The equivalent Greek letter is Delta, Δ. Architecture The minuscule (lower-case) form of 'd' consists of a lower-story left bowl and a stem ascender. It most likely developed by gradual variations on the majuscule (capital) form 'D', and today now composed as a stem with a full lobe to the right. In handwriting, it was common to start the arc to the left of the vertical stroke, resulting in a serif at the top of the arc. This seri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzimidazoles
Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a colorless solid. Preparation Benzimidazole is produced by condensation of o-phenylenediamine with formic acid,. or the equivalent trimethyl orthoformate: :C6H4(NH2)2 + HC(OCH3)3 → C6H4N(NH)CH + 3 CH3OH 2-substituted derivatives are obtained when the condensation is conducted with aldehydes in place of formic acid, followed by oxidation.Robert A. Smiley "Phenylene- and Toluenediamines" in Ullmann's Encyclopedia of Industrial Chemistry 2002, Wiley-VCH, Weinheim. Reactions Benzimidazole is a base: :C6H4N(NH)CH + H+ → 6H4(NH)2CHsup>+ It can also be deprotonated with stronger bases: :C6H4N(NH)CH + LiH → Li 6H4N2CH + H2 The imine can be alkylated and also serves as a ligand in coordination chemistry. The most prominent benzimidazole complex features ''N''-ribosyl-dimethylbenzimidazole as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
