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GR-159897
GR-159897 is a potent and selective NK2 receptor antagonist drug. It has anxiolytic effects in animal models, and also inhibits bronchoconstriction of the airways, which may potentially make it useful in the treatment of asthma. See also * Ibodutant * Nepadutant * Saredutant Saredutant (SR-48,968) is a drug that acts as a Tachykinin receptor 2, NK2 receptor receptor antagonist, antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to Phase III clinical trials, pha ... References Anxiolytics NK2 receptor antagonists Tryptamines Fluoroarenes Piperidines Ethers Sulfoxides {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachykinin Receptor 2
Substance-K receptor is a protein that in humans is encoded by the ''TACR2'' gene. Function This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A. Selective Ligands Several selective ligands for NK2 are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant. Agonists * GR-64349 - potent and selective agonist, EC50 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3 Antagonists * Ibodutant - failed its Phase 3 trial for IBS treatment in 2015, and abandoned by Menarini * Saredutant - mixed but ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bronchoconstriction
Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath. Causes The condition has a number of causes, the most common being emphysema as well as asthma. Exercise and allergies can bring on the symptoms in an otherwise asymptomatic individual. Emphysema With emphysema the shortness of breath due to effective bronchoconstriction from excessive very thick mucus blockage (it is so thick that great difficulty is encountered in expelling it resulting in near exhaustion at times) can bring on panic attacks unless the individual expects this and has effectively learned pursed lip breathing to more quickly transfer oxygen to the blood via the damaged alveoli resulting from the disease. The most common cause of emphysema is smoking and smoking cessation is mandatory if this incurable disease is to be treated. Prevention of bronchoconstriction by this pathway is vita ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
Ibodutant
Ibodutant was a candidate drug for irritable bowel syndrome diarrhea, developed by The Menarini Group. , it underwent a multicentre double blind efficacy clinical study. Ibodutant selectively blocks the tachykinin receptor NK2, with blockade practically complete in nano molar concentrations. A phase 2 trial in Europe (the IRIS-2 trial) completed in May 2012 with positive results. A 52-week phase 3 study was terminated as of 2015 because of low response and negative results of study NAK-06. See also * GR-159,897 * Nepadutant * Saredutant Saredutant (SR-48,968) is a drug that acts as a Tachykinin receptor 2, NK2 receptor receptor antagonist, antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to Phase III clinical trials, pha ... References Further reading * * Tachykinin receptor antagonists NK2 receptor antagonists Benzothiazoles Carboxamides Piperidines Tetrahydropyrans Cyclopentanes {{nervous- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nepadutant
Nepadutant (INN) (code name MEN-11420) is a glycosylated bicyclic cyclohexapeptide drug which acts as a highly selective NK2 receptor antagonist. It was developed by the Menarini Group and investigated for the treatment of functional gastrointestinal disorders and asthma but was never marketed. See also * GR-159,897 * Ibodutant * Saredutant Saredutant (SR-48,968) is a drug that acts as a Tachykinin receptor 2, NK2 receptor receptor antagonist, antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to Phase III clinical trials, pha ... References Acetamides Antispasmodics Bronchodilators Tryptamines NK2 receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saredutant
Saredutant (SR-48,968) is a drug that acts as a Tachykinin receptor 2, NK2 receptor receptor antagonist, antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to Phase III clinical trials, phase III clinical trials. However, in May 2009, Sanofi-Aventis published its quarterly results and announced the cessation of 14 research/development projects, among which was saredutant for the treatment of major depressive disorder. See also * GR-159,897 * Ibodutant * Nepadutant References 4-Phenylpiperidines Antidepressants Anxiolytics NK2 receptor antagonists Acetanilides Chloroarenes Benzamides Experimental drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytics
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NK2 Receptor Antagonists
NK may refer to: Businesses *Imerys (Euronext ticker code NK) *Nordiska Kompaniet, a department store in Stockholm, Sweden *Northrup-King Seed Company *Spirit Airlines (IATA code NK) *NK.pl, a Polish school-based social networking service Places *Nagorno-Karabakh Republic, a ''de facto'' state in the Nagorno-Karabakh region *Nikšić, Montenegro (license plate code NK) *North Kingstown, Rhode Island, United States **North Kingstown High School *North Korea, a common name for the Democratic People's Republic of Korea (DPRK) Other uses *Naik (military rank), rank in certain South Asian armies *Natural killer cell, in medicine *Neturei Karta, a group of anti-zionist orthodox Jews *Neue Kerze aka new candle, an old photometric unit of luminous intensity *Nippon Kaiji Kyokai, a classification society *Norwegian krone, a currency *NK (singer), a Ukrainian singer * NK, nogomentni klub, a football club in Croatian and Slovenian (e. g. NK Osijek, NK Maribor NK may refer to: Businesses *I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tryptamines
Substituted tryptamines, or serotonin analogues, are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino (NH2) group via an ethyl (−CH2–CH2−) sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and DMT. In South America, dimethyltryptamine is obtained from numerous plant sources, like chacruna, and it is often used in ayahuasca brews. Many synthetic tryptamines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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