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JNJ-42165279
JNJ-42165279 is a drug developed by Janssen Pharmaceutica which acts as a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 70 nM. It is described as a covalently binding but slowly reversible selective inhibitor of FAAH. JNJ-42165279 is being developed for the treatment of anxiety disorders and major depressive disorder. Clinical development has progressed as far as Phase II human trials with two studies in patients with mood disorders registered in ClinicalTrials.gov. In early 2016, a trial with a different FAAH inhibitor — Bial's BIA 10-2474 — resulted in a series of severe adverse events, including a death. In response, Janssen announced that it was temporarily suspending dosing in its two Phase II clinical trials with JNJ-42165279, describing the decision as "precautionary measure follows safety issue with different drug in class". Janssen was emphatic that no serious adverse events had been reported in any of th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Anxiolytics
This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. Generalized anxiety disorder * Agomelatine (AGO-178; Valdoxan) – melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist* Riluzole sublingual (BHV-0223) – undefined mechanism of action * TGFK08AA – 5-HT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BIA 10-2474
BIA 10-2474 is an experimental fatty acid amide hydrolase inhibitor developed by the Portuguese pharmaceutical company Bial-Portela & Ca. SA. It interacts with the human endocannabinoid system. The drug was in development for the treatment of a range of different medical conditions from anxiety disorder to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, cancer, hypertension or the treatment of obesity. A clinical trial with this drug was underway in Rennes, France, in January 2016, in which serious adverse events occurred affecting five participants, including the death of one man. The underlying mechanism that caused the acute neurotoxicity of this molecule remains unknown. Structure and action The chemical name of BIA-10-2474 is 3-(1-(cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide. BIA-10-2474 is a long-acting inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the centra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fatty Acid Amide Hydrolase
Fatty acid amide hydrolase or FAAH (, oleamide hydrolase, anandamide amidohydrolase) is a member of the serine hydrolase family of enzymes. It was first shown to break down anandamide in 1993. In humans, it is encoded by the gene ''FAAH''.; Function FAAH is an integral membrane hydrolase with a single ''N''-terminal transmembrane domain. ''In vitro'', FAAH has esterase and amidase activity. ''In vivo'', FAAH is the principal catabolic enzyme for a class of bioactive lipids called the fatty acid amides (FAAs). Members of the FAAs include: * Anandamide (''N''-arachidonoylethanolamine), an endocannabinoid * 2-arachidonoylglycerol (2-AG), an endocannabinoid. * Other ''N''-acylethanolamines, such as ''N''-oleoylethanolamine and ''N''-palmitoylethanolamine * The sleep-inducing lipid oleamide * The ''N''-acyltaurines, which are agonists of the transient receptor potential (TRP) family of calcium channels. ''FAAH'' knockout mice display highly elevated (>15-fold) levels of ''N'' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
URB-597
URB597 (KDS-4103) is a relatively selective and irreversible inhibitor of the enzyme fatty acid amide hydrolase (FAAH). FAAH is the primary degradatory enzyme for the endocannabinoid anandamide and, as such, inhibition of FAAH leads to an accumulation of anandamide in the CNS and periphery where it activates cannabinoid receptors. URB597 has been found to elevate anandamide levels and have activity against neuropathic pain in a mouse model. Preclinical studies have shown FAAH inhibitors to increase BDNF levels in the hippocampus and prefrontal cortex, highlighting their potential in addiction treatment as "enviromimetics". Indeed, Chauvet et al. found that chronic URB597 administration in rats "significantly reduces cocaine-seeking behaviour and cue- and stress-induced relapse". URB597 was at one point being developed by Kadmus Pharmaceuticals, Inc. for clinical trials in humans. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ureas
220 px, B vitamin, is a 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 intermediate: :COCl2 + R2NH → R2NC(O)Cl + HCl :COCl2 + RNH2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Inhibitors
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Reve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoids
Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary intoxicating compound in cannabis. Cannabidiol (CBD) is a major constituent of temperate Cannabis plants and a minor constituent in tropical varieties. At least 113 distinct phytocannabinoids have been isolated from cannabis, although only four (i.e., THCA, CBDA, CBCA and their common precursor CBGA) have been demonstrated to have a biogenetic origin. It was reported in 2020 that phytocannabinoids can be found in other plants such as rhododendron, licorice and liverwort, and earlier in Echinacea. Phytocannabinoids are multi-ring phenolic compounds structurally related to THC, but endocannabinoids are fatty acid derivatives. Nonclassical synthetic cannabinoids (cannabimimetics) include amin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PF-3845
PF-3845 is a selective inhibitor of fatty acid amide hydrolase. It results in increased levels of anandamide and results in cannabinoid receptor-based effects. It has anti-inflammatory action in mice colitis models. Antidiarrheal An anti-diarrhoeal drug (or anti-diarrheal drug in American English) is any medication which provides symptomatic relief for diarrhoea. Types * Electrolyte solutions, while not true antidiarrhoeals, are used to replace lost fluids and salts in ac ... and antinociceptive effects were also seen in mouse models of pain. A 2017 study published in the Journal of Psychiatry and Neuroscience found that PF-3845 exerts rapid and long-lasting anti-anxiety effects in mice exposed acutely to stress or chronically to the stress hormone corticosterone. References {{Cannabinoidergics Cannabinoids Experimental drugs Trifluoromethyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Janssen Pharmaceutica
Janssen Pharmaceuticals is a pharmaceutical company headquartered in Beerse, Belgium, and wholly-owned by Johnson & Johnson. It was founded in 1953 by Paul Janssen. In 1961, Janssen Pharmaceuticals was purchased by New Jersey-based American corporation Johnson & Johnson, and became part of Johnson & Johnson Pharmaceutical Research and Development (J&J PRD), now renamed to Janssen Research and Development (JRD), which conducts research and development activities related to a wide range of human medical disorders, including mental illness, neurological disorders, anesthesia and analgesia, gastrointestinal disorders, fungal infection, HIV/AIDS, allergies and cancer. Janssen and Ortho-McNeil Pharmaceutical have been placed in the Ortho-McNeil-Janssen group within Johnson & Johnson Company. Subsidiaries * Actelion * Cilag AG * Janssen Biotech (formerly ''Centocor'') * Janssen Vaccines (formerly ''Crucell'') * Tibotec * Beijing Dabao Cosmetics Co., Ltd. History The early roots ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-2183240
LY-2183240 is a drug which acts both as a potent inhibitor of the reuptake of the endocannabinoid anandamide and as an inhibitor of fatty acid amide hydrolase (FAAH), the primary enzyme responsible for degrading anandamide. This leads to markedly elevated anandamide levels in the brain, and LY-2183240 has been shown to produce both analgesic and anxiolytic effects in animal models. While LY-2183240 is a potent inhibitor of FAAH, it has relatively poor selectivity and also inhibits several other enzyme side targets. Consequently, it was never developed for clinical use, though it remains widely used in research, and has also been sold as a designer drug. See also *Endocannabinoid reuptake inhibitor * FAAH inhibitor ** BIA 10-2474 ** PF-04457845 ** URB-597 URB597 (KDS-4103) is a relatively selective and irreversible inhibitor of the enzyme fatty acid amide hydrolase (FAAH). FAAH is the primary degradatory enzyme for the endocannabinoid anandamide and, as such, inhibition of FAAH l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bial
Kempegowda International Airport is an international airport serving Bangalore, the capital of Karnataka, India. Spread over , it is located about north of the city near the suburb of Devanahalli. It is owned and operated by Bengaluru International Airport Limited (BIAL), a public–private consortium. The airport opened in May 2008 as an alternative to increased congestion at HAL Airport, the original primary commercial airport serving the city. It is named after Kempe Gowda I, the founder of Bangalore. Kempegowda International Airport became Karnataka's first fully solar powered airport developed by CleanMax Solar. Kempegowda International Airport is the third-busiest airport by passenger traffic, air traffic movements and domestic and total cargo handled in India, behind the airports in Delhi and Mumbai, and is the 29th busiest airport in Asia. In the FY 2021–22, the airport handled around 16.2 million passengers and of cargo. The airport has a single passen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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