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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] |
Menarini
The Menarini Group is an Italian pharmaceutical company. Its headquarters is in Florence, Tuscany, and it has three divisions: Menarini Ricerche, Menarini Biotech, and Menarini Diagnostics. It develops pharmacological solutions for cardiovascular diseases, oncology, pain/inflammation, asthma and anti-infectives. Menarini's research activities are carried out through Menarini Ricerche, which deals with all R&D activities, from the creation of new projects up to the drug registration. Its Menarini Biotech follows the creation of a biotechnological drug from the very early stages of research, through to the pilot scale and up to industrial production. The Group's Menarini Diagnostics division is a health care company with a worldwide network of affiliates partners and distributors focused on diabetes, haematology, clinical chemistry, urinalysis, and immunology. In 2020, the company had 17,650 employees worldwide. Massimiliana Landini Aleotti and her three children inherited the c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NK2 Receptor
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] |
GR-159,897
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] |
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] |
Irritable Bowel Syndrome
Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain and or abdominal bloating and changes in the consistency of bowel movements. These symptoms may occur over a long time, sometimes for years. IBS can negatively affect quality of life and may result in missed school or work (absenteeism) or reduced productivity at work (presenteeism). Disorders such as anxiety, major depression, and chronic fatigue syndrome are common among people with IBS.The cited review is based on sources ranging from 1988 to 2001 and is probably biased relative to a more recent research. The causes of IBS may well be multi-factorial. Theories include combinations of "gut–brain axis" problems, alterations in gut motility, visceral hypersensitivity, infections including small intestinal bacterial overgrowth, neurotransmitters, genetic factors, and food sensitivity. Onset may be triggered by an intestinal infec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, 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 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 studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachykinin Receptor
There are three known mammalian tachykinin receptors termed NK1, NK2 and NK3. All are members of the 7 transmembrane G-protein coupled receptor family and induce the activation of phospholipase C, producing inositol triphosphate (so called Gq-coupled). Inhibitors of NK-1, known as NK-1 receptor antagonists, can be used as antiemetic agents, such as the drug aprepitant. Binding The genes and receptor ligands are as follows: ( Hökfelt et al., 2001; Page, 2004; Pennefather et al., 2004; Maggi, 2000) See also *Substance P *G protein coupled receptor G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related p ...s References External links * * G protein-coupled receptors Molecular neuroscience {{biochem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Molar Concentration
Molar concentration (also called molarity, amount concentration or substance concentration) is a measure of the concentration of a chemical species, in particular of a solute in a solution, in terms of amount of substance per unit volume of solution. In chemistry, the most commonly used unit for molarity is the number of moles per liter, having the unit symbol mol/L or mol/ dm3 in SI unit. A solution with a concentration of 1 mol/L is said to be 1 molar, commonly designated as 1 M. Definition Molar concentration or molarity is most commonly expressed in units of moles of solute per litre of solution. For use in broader applications, it is defined as amount of substance of solute per unit volume of solution, or per unit volume available to the species, represented by lowercase c: :c = \frac = \frac = \frac. Here, n is the amount of the solute in moles, N is the number of constituent particles present in volume V (in litres) of the solution, and N_\text is the Av ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachykinin Receptor Antagonists
Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue. The tachykinin family is characterized by a common C-terminal sequence, Phe-X-Gly- Leu- Met-NH2, where X is either an Aromatic or an Aliphatic amino acid. The genes that produce tachykinins encode precursor proteins called preprotachykinins, which are chopped apart into smaller peptides by posttranslational proteolytic processing. The genes also code for multiple splice forms that are made up of different sets of peptides. Tachykinins excite neurons, evoke behavioral responses, are potent vasodilators, and contract (directly or indirectly) many smooth muscles. Tachykinins are from ten to twelve residues long. The two human tachykinin genes are called TAC1 and TAC3 for historical reasons, and are equivalent to Tac1 and Tac2 of the mouse, respectively. TAC1 encodes neurokinin A (formerly known as ... [...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] |
Benzothiazoles
Benzothiazole is an aromatic heterocyclic compound with the chemical formula . It is colorless, slightly viscous liquid. Although the parent compound, benzothiazole is not widely used, many of its derivatives are found in commercial products or in nature. Firefly luciferin can be considered a derivative of benzothiazole. Structure and preparation Benzothiazoles consist of a 5-membered 1,3-thiazole ring fused to a benzene ring. The nine atoms of the bicycle and the attached substituents are coplanar. Benzothiazoles are prepared by treatment of 2-mercaptoaniline with acid chlorides: :C6H4(NH2)SH + RC(O)Cl → C6H4(NH)SCR + HCl + H2O Uses Benzothiazole occurs naturally in some foods but is also used as a food additive. It has a sulfurous odor and meaty flavor. The European Food Safety Authority assessment had "no safety concern at estimated levels of intake as a flavouring substance". The heterocyclic core of the molecule is readily substituted at the unique methyne ce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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