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VUF-6002
VUF-6002 (JNJ-10191584) is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as o ... and analgesic effects in animal studies of inflammatory diseases. See also * JNJ-7777120 (same molecule but where one nitrogen has been exchanged for a carbon) References Benzimidazoles Piperazines Anti-inflammatory agents Johnson & Johnson brands H4 receptor antagonists Carboxamides Chloroarenes {{musculoskeletal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Histamine H4 Receptor
The histamine H4 receptor, like the other three histamine receptors, is a member of the G protein-coupled receptor superfamily that in humans is encoded by the ''HRH4'' gene. Discovery Unlike the histamine receptors discovered earlier, H4 was found in 2000 through a search of the human genomic DNA data base. Tissue distribution H4 is highly expressed in bone marrow and white blood cells and regulates neutrophil release from bone marrow and subsequent infiltration in the zymosan-induced pleurisy mouse model. It was also found that H4R exhibits a uniform expression pattern in the human oral epithelium. Function The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis. This occurs via the βγ subunit acting at phospholipase C to cause actin polymerization and eventually chemotaxis. Structure The 3D structure of the H4 receptor has not been solved yet due to the difficulties of GPCR crystallization. Some attempts have ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JNJ-7777120
JNJ-7777120 was a drug being developed by Johnson & Johnson Pharmaceutical Research & Development which acts as a potent and selective antagonist at the histamine H4 receptor. It has anti-inflammatory effects, and has been demonstrated to be superior to traditional (H1) antihistamines in the treatment of pruritus (itching). The drug was abandoned because of its short ''in vivo'' half-life and hypoadrenocorticism toxicity in rats and dogs, that prevented advancing it into clinical studies. See also * VUF-6002 VUF-6002 (JNJ-10191584) is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Ant ... References Carboxamides Chloroarenes H4 receptor antagonists Indoles Johnson & Johnson brands Piperazines Abandoned drugs {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Anti-inflammatory
Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as opposed to opioids, which affect the central nervous system to block pain signaling to the brain. Nonsteroidal anti-inflammatory drugs Nonsteroidal anti-inflammatory drugs (NSAIDs) alleviate pain by counteracting the cyclooxygenase (COX) enzyme. On its own, COX enzyme synthesizes prostaglandins, creating inflammation. In whole, the NSAIDs prevent the prostaglandins from ever being synthesized, reducing or eliminating the inflammation and resulting pain. Some common examples of NSAIDs are aspirin, ibuprofen, and naproxen. The newer specific COX-inhibitors are not classified together with the traditional NSAIDs, even though they presumably share the same mode of action. On the other hand, there are analgesics that are commonly associat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ... [...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 foun ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperazines
Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research. List of substituted piperazines Benzylpiperazines File:Benzylpiperazine.svg, 1-Benzylpiperazine File:MBZP.svg, 1-Methyl-4-benzylpiperazine File:DBZP.svg, 1,4-Dibenzylpiperazine File:MDBZP.svg, 3,4-Methylenedioxy-1-benzylpiperazine File:2C-B-BZP.svg, 4-Bromo-2,5-dimethoxy-1-benzylpiperazine File:Methoxypiperamide.png, Methoxypiperamide File:Sunifiram.svg , Sunifiram File:3-Methylbenzylpiperazine structure.png, 3-Methylbenzylpiperazine * 1-Benzylpiperazine (BZP) * 1-Methyl-4-benzylpiperazine (MBZP) * 1,4-Dibenzylpiperazine (DBZP) * 3,4-Methylenedioxy-1-benzylpiperazine (MDBZP) * 4-Bromo-2,5-dimethoxy-1-benzylpiperazine (2C-B-BZP) * Methoxypiperamide (MeOP, MEXP) ((4-methoxyphenyl)(4-methylpiperazin-1-yl)methanone) * Sunifiram (1-benzoyl-4-propanoylpiperazine) * 3-Methylbenzylpiperazine (3-MeBZP) Befuraline, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anti-inflammatory Agents
Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as opposed to opioids, which affect the central nervous system to block pain signaling to the brain. Nonsteroidal anti-inflammatory drugs Nonsteroidal anti-inflammatory drugs (NSAIDs) alleviate pain by counteracting the cyclooxygenase (COX) enzyme. On its own, COX enzyme synthesizes prostaglandins, creating inflammation. In whole, the NSAIDs prevent the prostaglandins from ever being synthesized, reducing or eliminating the inflammation and resulting pain. Some common examples of NSAIDs are aspirin, ibuprofen, and naproxen. The newer specific COX-inhibitors are not classified together with the traditional NSAIDs, even though they presumably share the same mode of action. On the other hand, there are analgesics that are commonly associated w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Johnson & Johnson Brands
Johnson is a surname of Anglo-Norman origin meaning "Son of John". It is the second most common in the United States and 154th most common in the world. As a common family name in Scotland, Johnson is occasionally a variation of ''Johnston'', a habitational name. Etymology The name itself is a patronym of the given name ''John'', literally meaning "son of John". The name ''John'' derives from Latin ''Johannes'', which is derived through Greek ''Iōannēs'' from Hebrew ''Yohanan'', meaning "Yahweh has favoured". Origin The name has been extremely popular in Europe since the Christian era as a result of it being given to St John the Baptist, St John the Evangelist and nearly one thousand other Christian saints. Other Germanic languages * Swedish: Johnsson, Jonsson * Icelandic: Jónsson See also * List of people with surname Johnson *Gjoni (Gjonaj) *Ioannou * Jensen *Johansson * Johns *Johnsson * Johnston *Johnstone *Jones *Jonson *Jonsson *Jovanović Jovanović ( sr-Cyr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H4 Receptor Antagonists
H4, H04, or H-4 may refer to: Science and mathematics * ATC code H04 ''Pancreatic hormones'', a subgroup of the Anatomical Therapeutic Chemical Classification System * Histamine H4 receptor, a human gene * Histone H4, a protein involved in the structure of chromatin in eukaryotic cells * Hydrogen-4 (H-4), an isotope of hydrogen * H4, a symmetry group in the fifth dimension. Technology * H-4 SOW, a precision-guided glide bomb used by the Pakistan Air Force * Halo 4, a video game created by 343 Industries for the Xbox 360 * Harrison Number Four, an 18th-century marine chronometer designed by John Harrison * Zoom H4 Handy Recorder, a handheld digital audio recorder * , level 4 heading markup for HTML Web pages, see HTML element#heading Transport Automobiles and roads * H4, a halogen headlamp bulb * H4, development name of the Hummer HX concept car * H-4, shorthand for a 4-cylinder horizontally-opposed or "flat four" engine (not to be confused with an actual H engine) * H4 Dans ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
