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Neurolixis
Neurolixis is a biopharmaceutical company focused on novel drugs for the treatment of human central nervous system diseases. Neurolixis Inc. was founded in 2011 by Mark A. Varney, PhD, and Adrian Newman-Tancredi, PhD, DSc. (Chief Executive Officer ). The company's therapeutic focus is on CNS disorders including Parkinson's disease, neurological orphan disorders, depression and cognitive deficits. The company has offices in USA and in France. In September 2013, Neurolixis in-licensed two clinical-phase drugs from Pierre Fabre Laboratories, a French pharmaceutical company. The drugs ( befiradol and F-15599) are targeted to the treatment of dyskinesia in Parkinson's disease and to breathing deficits in Rett syndrome, respectively. In addition, Neurolixis is developing its own novel chemical entities (NCEs). Neurolixis has been awarded a series of research grants by the Michael J. Fox Foundation and by Parkinson's UK. Neurolixis undertook research examining the effects of nove ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Befiradol
Befiradol (F-13,640; NLX-112) is an experimental drug being studied for the treatment of levodopa-induced dyskinesia. It is a potent and selective 5-HT1A receptor full agonist. Pharmacology In recombinant cell lines expressing human 5-HT1A receptors, befiradol exhibits high agonist efficacy for a variety of signal transduction read-outs, including ERK phosphorylation, G-protein activation, receptor internalization and adenylyl cyclase inhibition. In rat hippocampal membranes it preferentially activates GalphaO proteins. In neurochemical experiments, befiradol activated 5-HT1A autoreceptors in rat dorsal Raphe nucleus as well as 5-HT1A heteroreceptors on pyramidal neurons in the frontal cortex. It has powerful analgesic and antiallodynic effects comparable to those of high doses of opioid painkillers, but with fewer and less prominent side effects, as well as little or no development of tolerance with repeated use. A structure–activity relationship (SAR) study reveale ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
F-15599
F-15,599, also known as NLX-101, is a potent and selective 5-HT1A receptor full agonist. It displays functional selectivity (also known as "biased agonism") by strongly activating 5-HT1A receptors in the postsynaptic prefrontal cortex while having little effect on somatodendritic autoreceptors in the raphe nucleus. As a result, it has been touted as a preferential postsynaptic 5-HT1A receptor agonist and has been investigated as a novel potential antidepressant. In cognitive tests in rodent, F-15,599 attenuates memory deficits elicited by the NMDA receptor antagonist PCP, suggesting that it may improve cognitive function in disorders such as schizophrenia. A subsequent study showed that F-15,599 reduces breathing irregularity and apneas observed in mice with mutations of the MeCP2 gene. Dysruption of MeCP2 gene expression underlies Rett syndrome, a debilitating neurodevelopmental orphan disease. F-15,599 was discovered and initially developed by Pierre Fabre Médicament, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Central Nervous System
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all parts of the bodies of bilaterally symmetric and triploblastic animals—that is, all multicellular animals except sponges and diploblasts. It is a structure composed of nervous tissue positioned along the rostral (nose end) to caudal (tail end) axis of the body and may have an enlarged section at the rostral end which is a brain. Only arthropods, cephalopods and vertebrates have a true brain (precursor structures exist in onychophorans, gastropods and lancelets). The rest of this article exclusively discusses the vertebrate central nervous system, which is radically distinct from all other animals. Overview In vertebrates, the brain and spinal cord are both enclosed in the meninges. The meninges provide a barrier to chemicals d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
European Medicines Agency
The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or European Medicines Evaluation Agency (EMEA).Set up by EC Regulation No. 2309/93 as the European Agency for the Evaluation of Medicinal Products, and renamed by EC Regulation No. 726/2004 to the European Medicines Agency, it had the acronym EMEA until December 2009. The European Medicines Agency does not call itself EMA either – it has no official acronym but may reconsider if EMA becomes commonly accepted (secommunication on new visual identity an). The EMA was set up in 1995, with funding from the European Union and the pharmaceutical industry, as well as indirect subsidy from member states, its stated intention to harmonise (but not replace) the work of existing national medicine regulatory bodies. The hope was that this plan would not o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta Arrestin
Arrestins (abbreviated Arr) are a small family of proteins important for regulating signal transduction at G protein-coupled receptors. Arrestins were first discovered as a part of a conserved two-step mechanism for regulating the activity of G protein-coupled receptors (GPCRs) in the visual rhodopsin system by Hermann Kühn, Scott Hall, and Ursula Wilden and in the β-adrenergic system by Martin J. Lohse and co-workers. Function In response to a stimulus, GPCRs activate heterotrimeric G proteins. In order to turn off this response, or adapt to a persistent stimulus, active receptors need to be desensitized. The first step in desensitization is phosphorylation of the receptor by a class of serine/threonine kinases called G protein coupled receptor kinases (GRKs). GRK phosphorylation specifically prepares the activated receptor for arrestin binding. Arrestin binding to the receptor blocks further G protein-mediated signaling and targets receptors for internalization, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Extracellular Signal-regulated Kinases
In molecular biology, extracellular signal-regulated kinases (ERKs) or classical MAP kinases are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. Many different stimuli, including growth factors, cytokines, virus infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens, activate the ERK pathway. The term, "extracellular signal-regulated kinases", is sometimes used as a synonym for mitogen-activated protein kinase (MAPK), but has more recently been adopted for a specific subset of the mammalian MAPK family. In the MAPK/ERK pathway, Ras activates c-Raf, followed by mitogen-activated protein kinase kinase (abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below). Ras is typically activated by growth hormones through receptor tyrosine kinases and GRB2/SOS, but may also receive o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Jagiellonian University
The Jagiellonian University ( Polish: ''Uniwersytet Jagielloński'', UJ) is a public research university in Kraków, Poland. Founded in 1364 by King Casimir III the Great, it is the oldest university in Poland and the 13th oldest university in continuous operation in the world. It is regarded as Poland's most prestigious academic institution. The university has been viewed as a guardian of Polish culture, particularly for continuing operations during the partitions of Poland and the two World Wars, as well as a significant contributor to the intellectual heritage of Europe. The campus of the Jagiellonian University is centrally located within the city of Kraków. The university consists of thirteen main faculties, in addition to three faculties composing the Collegium Medicum. It employs roughly 4,000 academics and provides education to more than 35,000 students who study in 166 fields. The main language of instruction is Polish, although around 30 degrees are offered in Eng ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positron Emission Tomography
Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flow, regional chemical composition, and absorption. Different tracers are used for various imaging purposes, depending on the target process within the body. For example: * Fluorodeoxyglucose ( 18F">sup>18FDG or FDG) is commonly used to detect cancer; * 18Fodium fluoride">sup>18Fodium fluoride (Na18F) is widely used for detecting bone formation; * Oxygen-15 (15O) is sometimes used to measure blood flow. PET is a common imaging technique, a medical scintillography technique used in nuclear medicine. A radiopharmaceutical – a radioisotope attached to a drug – is injected into the body as a radioactive tracer, tracer. When the radiopharmaceutical undergoes beta plus decay, a positron is emitted, and when the positron interacts with an or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Functional Magnetic Resonance Imaging
Functional magnetic resonance imaging or functional MRI (fMRI) measures brain activity by detecting changes associated with blood flow. This technique relies on the fact that cerebral blood flow and neuronal activation are coupled. When an area of the brain is in use, blood flow to that region also increases. The primary form of fMRI uses the blood-oxygen-level dependent (BOLD) contrast, discovered by Seiji Ogawa in 1990. This is a type of specialized brain and body scan used to map neural activity in the brain or spinal cord of humans or other animals by imaging the change in blood flow ( hemodynamic response) related to energy use by brain cells. Since the early 1990s, fMRI has come to dominate brain mapping research because it does not involve the use of injections, surgery, the ingestion of substances, or exposure to ionizing radiation. This measure is frequently corrupted by noise from various sources; hence, statistical procedures are used to extract the underlying sig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Functional Selectivity
Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
University Of Bristol
The University of Bristol is a Red brick university, red brick Russell Group research university in Bristol, England. It received its royal charter in 1909, although it can trace its roots to a Society of Merchant Venturers, Merchant Venturers' school founded in 1595 and University College, Bristol, which had been in existence since 1876. Bristol is organised into #Academic structure, six academic faculties composed of multiple schools and departments running over 200 undergraduate courses, largely in the Tyndalls Park area of the city. The university had a total income of £752.0 million in 2020–21, of which £169.8 million was from research grants and contracts. It is the largest independent employer in Bristol. Current academics include 21 fellows of the Academy of Medical Sciences, 13 fellows of the British Academy, 13 fellows of the Royal Academy of Engineering and 44 fellows of the Royal Society. Among alumni and faculty, the university counts 9 Nobel laureates. Bristol is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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