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Fanapanel
Fanapanel (INN, code name ZK-200775), also known as MPQX, is a quinoxalinedione derivative drug which acts as a competitive antagonist of the AMPA receptor. It was under development by Schering AG for the treatment of cerebral ischemia associated with stroke and trauma, but clinical trials were halted for safety reasons related to possible glial cell toxicity and due to intolerable side effects such as excessive sedation, reduction in consciousness (consisting of stupor and coma), and transient neurological deterioration. The drug was also observed to produce visual alteration and impairment, including blurred vision, strongly impaired color perception, and reduced visual acuity and dark vision, side effects thought to be caused by blockade of AMPA receptors in the retina The retina (from la, rete "net") is the innermost, light-sensitive layer of tissue of the eye of most vertebrates and some molluscs. The optics of the eye create a focused two-dimensional image ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinoxalinedione
Quinoxalinedione is an organic compound with the formula C6H4(NH)2(CO)2. It is a colorless solid that is soluble in polar organic solvents. Quinoxalinediones are a family of related compounds sharing the same bicyclic core. Various quinoxalinediones are drugs. Synthesis and structure Quinoxalinedione is produced by condensation of dimethyloxalate and o-phenylenediamine: :C2O2(OMe)2 + C6H4(NH2)2 → C6H4(NH)2(CO)2 + 2 MeOH The compound exists in solution and the solid state predominantly as the diamide form. Some reactions of the compound indicate a role for the diol tautomer. Drugs based on quinoxalinediones Quinoxalinediones act as receptor antagonist, antagonists of the AMPA receptor, AMPA, kainate receptor, kainate, and/or NMDA receptors of the ionotropic glutamate receptor family. Examples include the following: * ACEA-1011 * Becampanel * CNQX * DNQX * Fanapanel (MPQX) * Licostinel (ACEA-1021) * NBQX * PNQX * YM90K * Zonampanel A drug closely related to the quinox ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMPA Receptor
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic transmembrane receptor for glutamate (iGluR) that mediates fast synaptic transmission in the central nervous system (CNS). It has been traditionally classified as a non-NMDA-type receptor, along with the kainate receptor. Its name is derived from its ability to be activated by the artificial glutamate analog AMPA. The receptor was first named the "quisqualate receptor" by Watkins and colleagues after a naturally occurring agonist quisqualate and was only later given the label "AMPA receptor" after the selective agonist developed by Tage Honore and colleagues at the Royal Danish School of Pharmacy in Copenhagen. The ''GRIA2''-encoded AMPA receptor ligand binding core (GluA2 LBD) was the first glutamate receptor ion channel domain to be crystallized. Structure and function Subunit composition AMPARs are composed of four types of subun ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Coma
A coma is a deep state of prolonged unconsciousness in which a person cannot be awakened, fails to respond normally to painful stimuli, light, or sound, lacks a normal wake-sleep cycle and does not initiate voluntary actions. Coma patients exhibit a complete absence of wakefulness and are unable to consciously feel, speak or move. Comas can be derived by natural causes, or can be medically induced. Clinically, a coma can be defined as the inability consistently to follow a one-step command. It can also be defined as a score of ≤ 8 on the Glasgow Coma Scale (GCS) lasting ≥ 6 hours. For a patient to maintain consciousness, the components of ''wakefulness'' and ''awareness'' must be maintained. Wakefulness describes the quantitative degree of consciousness, whereas awareness relates to the qualitative aspects of the functions mediated by the cortex, including cognitive abilities such as attention, sensory perception, explicit memory, language, the execution of tasks, temporal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluoromethyl Compounds
The trifluoromethyl group is a functional group that has the formula -CF3. The naming of is group is derived from the methyl group (which has the formula -CH3), by replacing each hydrogen atom by a fluorine atom. Some common examples are trifluoromethane H–, 1,1,1-trifluoroethane –, and hexafluoroacetone –CO–. Compounds with this group are a subclass of the organofluorines. Properties The trifluoromethyl group has a significant electronegativity that is often described as being intermediate between the electronegativities of fluorine and chlorine. For this reason, trifluoromethyl-substituted compounds are often strong acids, such as trifluoromethanesulfonic acid and trifluoroacetic acid. Conversely, the trifluoromethyl group lowers the basicity of compounds like trifluoroethanol. Uses The trifluoromethyl group occurs in certain pharmaceuticals, drugs, and abiotically synthesized natural fluorocarbon based compounds. The medicinal use of the trifloromethyl group dates f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuroprotective Agents
Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal loss over time, which can be expressed as a differential equation. It is a widely explored treatment option for many central nervous system (CNS) disorders including neurodegenerative diseases, stroke, traumatic brain injury, spinal cord injury, and acute management of neurotoxin consumption (i.e. methamphetamine overdoses). Neuroprotection aims to prevent or slow disease progression and secondary injuries by halting or at least slowing the loss of neurons. Despite differences in symptoms or injuries associated with CNS disorders, many of the mechanisms behind neurodegeneration are the same. Common mechanisms of neuronal injury include decreased delivery of oxygen and glucose to the brain, energy failure, increased levels in oxidative stre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMPA Receptor Antagonists
α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, better known as AMPA, is a compound that is a specific agonist for the AMPA receptor, where it mimics the effects of the neurotransmitter glutamate. There are several types of glutamatergic ion channels in the central nervous system including AMPA, kainic acid and ''N''-methyl-D-aspartic acid (NMDA) channels. In the synapse, these receptors serve very different purposes. AMPA can be used experimentally to distinguish the activity of one receptor from the other in order to understand their differing functions. AMPA generates fast excitatory postsynaptic potentials (EPSP). AMPA activates AMPA receptors that are non-selective cationic channels allowing the passage of Na+ and K+ and therefore have an equilibrium potential near 0 mV. AMPA was first synthesized, along with several other ibotenic acid derivatives, by Krogsgaard-Larsen, Honoré, and others toward differentiating glutamate sensitive receptors from aspartate sen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Retina
The retina (from la, rete "net") is the innermost, light-sensitive layer of tissue of the eye of most vertebrates and some molluscs. The optics of the eye create a focused two-dimensional image of the visual world on the retina, which then processes that image within the retina and sends nerve impulses along the optic nerve to the visual cortex to create visual perception. The retina serves a function which is in many ways analogous to that of the film or image sensor in a camera. The neural retina consists of several layers of neurons interconnected by synapses and is supported by an outer layer of pigmented epithelial cells. The primary light-sensing cells in the retina are the photoreceptor cells, which are of two types: rods and cones. Rods function mainly in dim light and provide monochromatic vision. Cones function in well-lit conditions and are responsible for the perception of colour through the use of a range of opsins, as well as high-acuity vision used fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dark Vision
Night vision is the ability to see in low-light conditions, either naturally with scotopic vision or through a night-vision device. Night vision requires both sufficient spectral range and sufficient intensity range. Humans have poor night vision compared to many animals such as cats, foxes and rabbits, in part because the human eye lacks a tapetum lucidum, tissue behind the retina that reflects light back through the retina thus increasing the light available to the photoreceptors. Types of ranges Spectral range Night-useful spectral range techniques can sense radiation that is invisible to a human observer. Human vision is confined to a small portion of the electromagnetic spectrum called visible light. Enhanced spectral range allows the viewer to take advantage of non-visible sources of electromagnetic radiation (such as near-infrared or ultraviolet radiation). Some animals such as the mantis shrimp and trout can see using much more of the infrared and/or ultraviolet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Visual Acuity
Visual acuity (VA) commonly refers to the clarity of vision, but technically rates an examinee's ability to recognize small details with precision. Visual acuity is dependent on optical and neural factors, i.e. (1) the sharpness of the retinal image within the eye, (2) the health and functioning of the retina, and (3) the sensitivity of the interpretative faculty of the brain. The most commonly referred visual acuity is the far acuity (e.g. 6/6 or 20/20 acuity), which describes the examinee's ability to recognize small details at a far distance, and is relevant to people with myopia; however, for people with hyperopia, the near acuity is used instead to describe the examinee's ability to recognize small details at a near distance. A common cause of low visual acuity is refractive error (ametropia), errors in how the light is refracted in the eyeball, and errors in how the retinal image is interpreted by the brain. The latter is the primary cause for low vision in people with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Color Perception
Color vision, a feature of visual perception, is an ability to perceive differences between light composed of different wavelengths (i.e., different spectral power distributions) independently of light intensity. Color perception is a part of the larger visual system and is mediated by a complex process between neurons that begins with differential stimulation of different types of photoreceptors by light entering the eye. Those photoreceptors then emit outputs that are propagated through many layers of neurons and then ultimately to the brain. Color vision is found in many animals and is mediated by similar underlying mechanisms with common types of biological molecules and a complex history of evolution in different animal taxa. In primates, color vision may have evolved under selective pressure for a variety of visual tasks including the foraging for nutritious young leaves, ripe fruit, and flowers, as well as detecting predator camouflage and emotional states in other pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
