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SB-705498
SB-705498 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel. It has been evaluated in clinical trials for the treatment of rhinitis and chronic cough. See also * AMG-517 * AMG-9810 * Discovery and development of TRPV1 antagonists Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new anesthetic, analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor (biochemistry), receptor is a ligand gat ... References Ureas Trifluoromethyl compounds Disubstituted pyridines 2-Bromophenyl compounds Pyrrolidines Transient receptor potential channel modulators {{respiratory-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TRPV1
The transient receptor potential cation channel subfamily V member 1 (TRPV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the ''TRPV1'' gene. It was the first isolated member of the transient receptor potential vanilloid receptor proteins that in turn are a sub-family of the transient receptor potential protein group. This protein is a member of the TRPV group of Transient receptor potential channel, transient receptor potential family of ion channels. Fatty acid Fatty acid metabolism, metabolites with affinity for this receptor are produced by cyanobacteria, which Divergent evolution, diverged from eukaryotes at least 2billion years ago. The function of TRPV1 is detection and regulation of body temperature. In addition, TRPV1 provides a sensation of scalding heat and pain (nociception). In primary afferent sensory neurons, it cooperates with TRPA1 (a chemical irritant receptor) to mediate the detection of noxio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMG-517
AMG-517 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel. It was developed as a potential treatment for chronic pain, but while it was an effective analgesic in animal studies it was dropped from human clinical trials at Phase I due to producing hyperthermia as a side effect, as well as poor water solubility. It is still used in scientific research into the function of the TRPV1 channel and its role in pain and inflammation, and has been used as a template for the design of several newer analogues which have improved properties. See also * AMG-9810 * SB-705498 * Discovery and development of TRPV1 antagonists Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new anesthetic, analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor (biochemistry), receptor is a ligand gat ... References Benzothiazoles {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMG-9810
AMG-9810 is a drug which acts as a potent and selective antagonist for the TRPV1 receptor. It has analgesic and antiinflammatory effects and is used in scientific research, but has not been developed for medical use. It has high antagonist potency and good bioavailability and pharmacokinetics, and so has been used to study the role of TRPV1 in areas other than pain perception, such as its roles in the brain. See also * AMG-517 * SB-705498 SB-705498 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel. It has been evaluated in clinical trials for the treatment of rhinitis and chronic cough. See also * AMG-517 * AMG-9810 * Discovery and development of ... References Benzodioxans Transient receptor potential channel modulators {{musculoskeletal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Discovery And Development Of TRPV1 Antagonists
Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new anesthetic, analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor (biochemistry), receptor is a ligand gated ion channel that has been implicated in mediation of many types of pain and therefore studied most extensively. The first competitive antagonist, capsazepine, was first described in 1990; since then, several TRPV1 antagonists have entered clinical trials as analgesic agents. Should these new chemical entities relieve symptoms of chronic pain, then this class of compounds may offer one of the first novel mechanisms for the treatment of pain in many years. History Capsaicin, the active ingredient in chili pepper, was first isolated over a century ago. In 1919 the exact chemical structure of capsaicin was determined and the complete synthesis of the compound was achieved a decade later. Capsaicin has been used as an analgesic for decades ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ion Channel
Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore. Their functions include establishing a resting membrane potential, shaping action potentials and other electrical signals by Gating (electrophysiology), gating the flow of ions across the cell membrane, controlling the flow of ions across secretion, secretory and epithelial cells, and regulating cell (biology), cell volume. Ion channels are present in the membranes of all cells. Ion channels are one of the two classes of ionophore, ionophoric proteins, the other being ion transporters. The study of ion channels often involves biophysics, electrophysiology, and pharmacology, while using techniques including voltage clamp, patch clamp, immunohistochemistry, X-ray crystallography, fluoroscopy, and RT-PCR. Their classification as molecules is referred to as channelomics. Basic features There are two distinctive features of ion channels that differentiate them from other types of ion ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rhinitis
Rhinitis, also known as coryza, is irritation and inflammation of the mucous membrane inside the nose. Common symptoms are a stuffy nose, runny nose, sneezing, and post-nasal drip. The inflammation is caused by viruses, bacteria, irritants or allergens. The most common kind of rhinitis is allergic rhinitis, which is usually triggered by airborne allergens such as pollen and dander. Allergic rhinitis may cause additional symptoms, such as sneezing and nasal itching, coughing, headache, fatigue, malaise, and cognitive impairment. The allergens may also affect the eyes, causing watery, reddened, or itchy eyes and puffiness around the eyes. The inflammation results in the generation of large amounts of mucus, commonly producing a runny nose, as well as a stuffy nose and post-nasal drip. In the case of allergic rhinitis, the inflammation is caused by the degranulation of mast cells in the nose. When mast cells degranulate, they release histamine and other chemicals, starting ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chronic Cough
In clinical guidelines chronic cough is defined as a cough lasting more than 8 weeks in adults and more than 4 weeks in children. Some consensus statements suggest that a chronic cough must persist upwards of three months or more to be considered chronic. The prevalence of chronic cough is about 10% although the prevalence may differ depending on definition and geographic area. Chronic cough is a common symptom in several different respiratory diseases like COPD or pulmonary fibrosis but in non-smokers with a normal chest x-ray chronic cough are often associated with asthma, rhinosinusitis, and gastroesophageal reflux disease or could have no specific cause known ( idiopathic). Generally, a cough, for example after an upper respiratory tract infection, lasts around one to two weeks; however, chronic cough can persist for an extended period of time, several years in some cases. The current theory about the cause of chronic cough, independent of associated condition, is that it is ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ureas
image:Biotin_structure.svg, 220 px, Biotin, a water-soluble B vitamins, B vitamin, is a bicyclic urea. In chemistry, ureas are a class of organic compounds with the formula (R2N)2CO where R = H, alkyl, aryl, etc. Thus, in addition to describing the specific chemical compound urea ((H2N)2CO), urea is the name of a functional group that is found in many compounds and materials of both practical and theoretical interest. Generally ureas are colorless crystalline solids, which, owing to the presence of fewer hydrogen bonds, exhibit melting points lower than that of urea itself. Synthesis Ureas can be prepared many methods, but rarely by direct carbonation, which is the route to urea itself. Instead, methods can be classified according those that assemble the urea functionality and those that start with preformed urea. Assembly of N-substituted urea functionality Phosgenation entails the reaction of amines with phosgene, proceeding via the isocyanate (or carbamoyl chloride) as an i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluoromethyl Compounds
The trifluoromethyl group is a functional group that has the formula In science, a formula is a concise way of expressing information symbolically, as in a mathematical formula or a ''chemical formula''. The informal use of the term ''formula'' in science refers to the general construct of a relationship betwe ... . The naming of is group is derived from the methyl group (which has the formula ), by replacing each hydrogen atom by a fluorine atom. Some common examples are trifluoromethane , 1,1,1-trifluoroethane , and hexafluoroacetone . Compounds with this group are a subclass of the organofluorines. Properties The trifluoromethyl group has a significant electronegativity that is often described as being intermediate between the electronegativities of fluorine and chlorine. For this reason, trifluoromethyl-substituted compounds are often strong acids, such as trifluoromethanesulfonic acid and trifluoroacetic acid. Conversely, the trifluoromethyl group lowers the basicity of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
