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Toreforant
Toreforant (JNJ-38518168) is an orally-dosed selective antagonist of the histamine H4 receptor that has been studied for various health conditions. It is the successor of a number of H4-selective compounds developed by Johnson & Johnson. Phase IIa clinical trials completed as recently as November 2018 continue to suggest that toreforant is safe. As of the end of 2020, there is no regulator-approved H4 antagonist. In U.S. Phase II clinical trials, toreforant, by itself, did not show efficacy against eosinophilic asthma. The drug did show at least partial efficacy against rheumatoid arthritis in patients who were nonresponsive to methotrexate. As the H4 receptor is widely implicated in the regulation of inflammatory states, the potential uses for an H4 antagonist remain significant. See also * 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 recept ... [...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] |
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, |
Johnson & Johnson
Johnson & Johnson (J&J) is an American multinational corporation founded in 1886 that develops medical devices, pharmaceuticals, and consumer packaged goods. Its common stock is a component of the Dow Jones Industrial Average and the company is ranked No. 36 on the 2021 Fortune 500 list of the largest United States corporations by total revenue. Johnson & Johnson is one of the List of public corporations by market capitalization, world's most valuable companies, and is one of only two U.S.-based companies that has a prime credit rating of AAA, higher than that of the United States government. Johnson & Johnson is headquartered in New Brunswick, New Jersey, the consumer division being located in Skillman, New Jersey. The corporation includes some 250 subsidiary companies with operations in 60 countries and products sold in over 175 countries. Johnson & Johnson had worldwide sales of $93.8billion during calendar year 2021. Johnson & Johnson's brands include numerous household na ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eosinophilic Asthma
Asthma is a long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, coughing, chest tightness, and shortness of breath. These may occur a few times a day or a few times per week. Depending on the person, asthma symptoms may become worse at night or with exercise. Asthma is thought to be caused by a combination of genetic and environmental factors. Environmental factors include exposure to air pollution and allergens. Other potential triggers include medications such as aspirin and beta blockers. Diagnosis is usually based on the pattern of symptoms, response to therapy over time, and spirometry lung function testing. Asthma is classified according to the frequency of symptoms, forced expiratory volume in one second (FEV1), and peak expiratory flow rate. It may also be classified as atopic or non-atopic, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rheumatoid Arthritis
Rheumatoid arthritis (RA) is a long-term autoimmune disorder that primarily affects joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and hands are involved, with the same joints typically involved on both sides of the body. The disease may also affect other parts of the body, including skin, eyes, lungs, heart, nerves and blood. This may result in a low red blood cell count, inflammation around the lungs, and inflammation around the heart. Fever and low energy may also be present. Often, symptoms come on gradually over weeks to months. While the cause of rheumatoid arthritis is not clear, it is believed to involve a combination of genetic and environmental factors. The underlying mechanism involves the body's immune system attacking the joints. This results in inflammation and thickening of the joint capsule. It also affects the underlying bone and cartilage. The diagnosis is made mos ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methotrexate
Methotrexate (MTX), formerly known as amethopterin, is a chemotherapy agent and immune-system suppressant. It is used to treat cancer, autoimmune diseases, and ectopic pregnancies. Types of cancers it is used for include breast cancer, leukemia, lung cancer, lymphoma, gestational trophoblastic disease, and osteosarcoma. Types of autoimmune diseases it is used for include psoriasis, rheumatoid arthritis, and Crohn's disease. It can be given by mouth or by injection. Common side effects include nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth. Other side effects may include liver disease, lung disease, lymphoma, and severe skin rashes. People on long-term treatment should be regularly checked for side effects. It is not safe during breastfeeding. In those with kidney problems, lower doses may be needed. It acts by blocking the body's use of folic acid. Methotrexate was first made in 1947 and ... [...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] |
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] |
