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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 Addison's disease, also known as primary adrenal insufficiency, is a rare long-term endocrine disorder characterized by inadequate production of the steroid hormones cortisol and aldosterone by the two outer layers of the cells of the adrenal ... toxicity in rats and dogs, that prevented advancing it into clinical studies. See also * VUF-6002 References Carboxamides Chloroarenes H4 receptor antagonists Indoles Johnson & Johnson brands Piperazines Abandoned drugs {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Johnson & Johnson Pharmaceutical Research & Development
Johnson & Johnson Pharmaceutical Research and Development (J&JPRD) is a subsidiary of Johnson & Johnson that is responsible for drug discovery, discovering and drug development, developing pharmaceutical drugs. J&JPRD has research sites located in Raritan, New Jersey, Titusville, New Jersey, Spring House, Pennsylvania, La Jolla, California, Beerse, Belgium and Toledo, Spain. J&JPRD was created in 2001 through the merging of various research organizations including McNeil Pharmaceuticals, Janssen Pharmaceutica, Janssen Research Foundation, Three Dimensional Pharmaceuticals, and the R. W. Johnson Pharmaceutical Research Institute. Research Collaborative In addition to internal research and development activities J&JPRD is also involved in publicly funded collaborative research projects, with other industrial and academic partners. One example in the area of Pre-clinical development, non-clinical safety assessment is the InnoMed PredTox. The company is expanding its activities in joi ... [...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, beta blocker [...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] |
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 associated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pruritus
Itch (also known as pruritus) is a sensation that causes the desire or reflex to scratch. Itch has resisted many attempts to be classified as any one type of sensory experience. Itch has many similarities to pain, and while both are unpleasant sensory experiences, their behavioral response patterns are different. Pain creates a withdrawal reflex, whereas itch leads to a scratch reflex. Unmyelinated nerve fibers for itch and pain both originate in the skin; however, information for them is conveyed centrally in two distinct systems that both use the same nerve bundle and spinothalamic tract. Classification Most commonly, an itch is felt in one place. If it is felt all over the body, then it is called ''generalized itch'' or ''generalized pruritus''. If the sensation of itching persists for six weeks or longer, then it is called ''chronic itch'' or ''chronic pruritus''. ''Chronic idiopathic pruritus'' or ''essential pruritus'' is a rare form of itch that persists for longer t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vivo
Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, and plants, as opposed to a tissue extract or dead organism. This is not to be confused with experiments done ''in vitro'' ("within the glass"), i.e., in a laboratory environment using test tubes, Petri dishes, etc. Examples of investigations ''in vivo'' include: the pathogenesis of disease by comparing the effects of bacterial infection with the effects of purified bacterial toxins; the development of non-antibiotics, antiviral drugs, and new drugs generally; and new surgical procedures. Consequently, animal testing and clinical trials are major elements of ''in vivo'' research. ''In vivo'' testing is often employed over ''in vitro'' because it is better suited for observing the overall effects of an experiment on a living subject. In ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biological Half-life
Biological half-life (also known as elimination half-life, pharmacologic half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma, and is denoted by the abbreviation t_. This is used to measure the removal of things such as metabolites, drugs, and signalling molecules from the body. Typically, the biological half-life refers to the body's natural cleansing through the function of the liver and through the excretion of the measured substance through the kidneys and intestines. This concept is used when the rate of removal is roughly exponential. In a medical context, half-life explicitly describes the time it takes for the blood plasma concentration of a substance to halve (''plasma half-life'') its steady-state when circulating in the full blood of an organism. This measurement is useful in medicine, pharmacology and pharmacokinetics because it helps ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypoadrenocorticism
Addison's disease, also known as primary adrenal insufficiency, is a rare long-term endocrine disorder characterized by inadequate production of the steroid hormones cortisol and aldosterone by the two outer layers of the cells of the adrenal glands (adrenal cortex), causing adrenal insufficiency. Symptoms generally come on slowly and insidiously and may include abdominal pain and gastrointestinal abnormalities, weakness, and weight loss. Hyperpigmentation, Darkening of the skin in certain areas may also occur. Under certain circumstances, an adrenal crisis may occur with shock (circulatory), low blood pressure, vomiting, lower back pain, and Coma, loss of consciousness. Mood changes may also occur. Rapid onset of symptoms indicates acute adrenal failure which is a serious and emergent condition. An adrenal crisis can be triggered by stress, such as from an injury, surgery, or infection. Addison's disease arises from problems with the adrenal gland such that not enough of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
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 of ... [...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] |
