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BNC-210
BNC210 (also known as IW-2143 during its time licensed to Ironwood Pharmaceuticals) is an anxiolytic drug that acts via negative allosteric modulation of the α7-nicotinic acetylcholine receptor, by Bionomics Limited. It is currently being investigated for the treatment of post traumatic stress disorder. The drug has demonstrated clinically significant anxiety reduction in both animal models and in Phase I trials. It appears to be devoid of significant sedation or memory-impairing side effects, as well as lacking addictive potential in rat discriminatory models. Phase I trials have shown no serious side effects. Bionomics previously licensed it to Ironwood Pharmaceuticals in January 2012, where it was known as IW-2143. In December 2012, IW-2143 begun undergoing phase I clinical trials in the United States, but in November 2014, was released back to Bionomics in a mutual agreement. Bionomics will now continue development and clinical testing, with Ironwood receiving a royalt ... [...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] |
Ironwood Pharmaceuticals
Ironwood Pharmaceuticals, Inc is a publicly traded pharmaceutical company. It was originally called Microbia, Inc. Microbia was founded by postdocs from the lab of Gerald Fink at the Whitehead Institute to commercialize approaches that had been developed in the lab to improve industrial fermentation of fungi, to genetically engineer them to produce secondary metabolites more efficiently or to produce new ones as leads for drug discovery or as products for use in industry, and to identify drug targets in fungi for antifungal drug discovery. In 2002 the company hired John Talley to lead their antifungal drug discovery efforts, which at the time were focused on identifying small molecules that could inhibit fungal invasins, along with Mark Currie who had also worked at Searle division of Monsanto with Talley, and then had gone to Sepracor, and also Richard Bailey, who had run Monsanto's nutritional business. Currie directed the efforts that led to the discovery of linaclotide, wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetylcholine
Acetylcholine (ACh) is an organic chemical that functions in the brain and body of many types of animals (including humans) as a neurotransmitter. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Parts in the body that use or are affected by acetylcholine are referred to as cholinergic. Substances that increase or decrease the overall activity of the cholinergic system are called cholinergics and anticholinergics, respectively. Acetylcholine is the neurotransmitter used at the neuromuscular junction—in other words, it is the chemical that motor neurons of the nervous system release in order to activate muscles. This property means that drugs that affect cholinergic systems can have very dangerous effects ranging from paralysis to convulsions. Acetylcholine is also a neurotransmitter in the autonomic nervous system, both as an internal transmitter for the sympathetic nervous system and as the final product released by the parasymp ... [...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] |
Dipeptides
A dipeptide is an organic compound derived from two amino acids. The constituent amino acids can be the same or different. When different, two isomers of the dipeptide are possible, depending on the sequence. Several dipeptides are physiologically important, and some are both physiologically and commercially significant. A well known dipeptide is aspartame, an artificial sweetener. Dipeptides are white solids. Many are far more water-soluble than the parent amino acids. For example, the dipeptide Ala-Gln has the solubility of 586 g/L more than 10x the solubility of Gln (35 g/L). Dipeptides also can exhibit different stabilities, e.g. with respect to hydrolysis. Gln does not withstand sterilization procedures, whereas this dipeptide does. Because dipeptides are prone to hydrolysis, the high solubility is exploited in infusions, i.e. to provide nutrition. Examples Commercial value About six dipeptides are of commercial interest. *Aspartame (''N''-L-α-aspartyl-L-phenyla ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kynurenic Acid
Kynurenic acid (KYNA or KYN) is a product of the normal metabolism of amino acid -tryptophan. It has been shown that kynurenic acid possesses neuroactive activity. It acts as an antiexcitotoxic and anticonvulsant, most likely through acting as an antagonist at excitatory amino acid receptors. Because of this activity, it may influence important neurophysiological and neuropathological processes. As a result, kynurenic acid has been considered for use in therapy in certain neurobiological disorders. Conversely, increased levels of kynurenic acid have also been linked to certain pathological conditions. Kynurenic acid was discovered in 1853 by the German chemist Justus von Liebig in dog urine, which it was apparently named after.Liebig, J., Uber Kynurensäure, ''Justus Liebigs Ann. Chem.'', 86: 125-126, 1853. It is formed from -kynurenine in a reaction catalyzed by the enzyme kynurenine—oxoglutarate transaminase. Mechanism of action KYNA has been proposed to act on five targe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Hydroxyindoleacetic Acid
5-Hydroxyindoleacetic acid (5-HIAA) is the main metabolite of serotonin. In chemical analysis of urine samples, 5-HIAA is used to determine serotonin levels in the body. Clinical significance 5-HIAA is tested by 24-hour urine samples combined with an acidic additive to maintain pH below 3. Certain foods like pineapple, kiwi, banana, walnuts and drugs such as acetaminophen, nicotine or caffeine are known to interfere with the measurement. 5-HIAA levels can vary depending on other complications, including tumors, renal malfunction, and small bowel resection. Since 5-HIAA is a metabolite of serotonin, testing is most frequently performed for the diagnosis of carcinoid tumors of the enterochromaffin (Kultschitzsky) cells of the small intestine, which release large amounts of serotonin. Values greater than 25 mg per 24 hours (higher if the patient has malabsorption) are strong evidence for carcinoid. The normal range is 2 to 6 mg per 24 hours. Low levels of 5-HIAA in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Efficacy
Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as ''effectiveness'', and it has often been used synonymously, although in pharmacology a pragmatic clinical trial#Efficacy versus effectiveness, distinction is now often made between efficacy and effectiveness. The word ''efficacy'' is used in pharmacology and medicine to refer both to the maximum response achievable from a pharmaceutical drug in research settings, and to the capacity for sufficient therapeutic effect or beneficial change in clinical settings. Pharmacology In pharmacology, efficacy () is the maximum response achievable from an applied or dosed agent, for instance, a small molecule drug. Intrinsic activity is a relative term for a drug's efficacy relative to a drug with the highest observed efficacy. It is a purely descriptive term that has little or no mechanistic interpretation. In order for a drug to have an effect, it needs to bind to its t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorazepam
Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication. It is used to treat anxiety disorders, trouble sleeping, severe agitation, active seizures including status epilepticus, alcohol withdrawal, and chemotherapy-induced nausea and vomiting. It is also used during surgery to interfere with memory formation and to sedate those who are being mechanically ventilated. It is also used, along with other treatments, for acute coronary syndrome due to cocaine use. It can be given by mouth or as an injection into a muscle or vein. When given by injection onset of effects is between one and thirty minutes and effects last for up to a day. Common side effects include weakness, sleepiness, low blood pressure, and a decreased effort to breathe. When given intravenously the person should be closely monitored. Among those who are depressed there may be an increased risk of suicide. With long-term use, larger doses may be required for the same ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CHRNA7
Neuronal acetylcholine receptor subunit alpha-7, also known as nAChRα7, is a protein that in humans is encoded by the ''CHRNA7'' gene. The protein encoded by this gene is a subunit of certain nicotinic acetylcholine receptors (nAchR). Function The nicotinic acetylcholine receptors (nAChRs) are members of a superfamily of ligand-gated ion channels that mediate fast signal transmission at synapses. The nAChRs are thought to be hetero-pentamers composed of homologous subunits. The proposed structure for each subunit is a conserved N-terminal extracellular domain followed by three conserved transmembrane domains, a variable cytoplasmic loop, a fourth conserved transmembrane domain, and a short C-terminal extracellular region. The protein encoded by this gene forms a homo-oligomeric channel, displays marked permeability to calcium ions and is a major component of brain nicotinic receptors that are blocked by, and highly sensitive to, alpha-bungarotoxin. Once this receptor binds acety ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Post-traumatic Stress Disorder
Post-traumatic stress disorder (PTSD) is a mental and behavioral disorder that can develop because of exposure to a traumatic event, such as sexual assault, warfare, traffic collisions, child abuse, domestic violence, or other threats on a person's life. Symptoms may include disturbing thoughts, feelings, or dreams related to the events, mental or physical distress to trauma-related cues, attempts to avoid trauma-related cues, alterations in the way a person thinks and feels, and an increase in the fight-or-flight response. These symptoms last for more than a month after the event. Young children are less likely to show distress but instead may express their memories through play. A person with PTSD is at a higher risk of suicide and intentional self-harm. Most people who experience traumatic events do not develop PTSD. People who experience interpersonal violence such as rape, other sexual assaults, being kidnapped, stalking, physical abuse by an intimate partner, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Traumatic Stress
Traumatic stress is a common term for reactive anxiety and depression, although it is not a medical term and is not included in the ''Diagnostic and Statistical Manual of Mental Disorders'' (DSM). The experience of traumatic stress include subtypes of anxiety, depression and disturbance of conduct along with combinations of these symptoms. This may result from events that are less threatening and distressing than those that lead to post-traumatic stress disorder. The fifth edition of the DSM describes in a section titled "Trauma and Stress-Related Disorders" disinhibited social engagement disorder, reactive attachment disorder, acute stress disorder, adjustment disorder, and post-traumatic stress disorder. Symptoms Symptoms of traumatic stress can be both physical and emotional. Physical symptoms include trembling, shaking, a pounding heart, rapid breathing, choking feelings, stomach tightening/churning, dizziness/faintness, and cold sweats. Emotional symptoms include racing tho ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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