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7-Chlorokynurenic Acid
7-Chlorokynurenic acid (7-CKA) is a tool compound that acts as a potent and selective competitive antagonist of the glycine site of the NMDA receptor. It produces ketamine-like rapid antidepressant effects in animal models of depression. However, 7-CKA is unable to cross the blood-brain-barrier, and for this reason, is unsuitable for clinical use. As a result, a centrally-penetrant prodrug of 7-CKA, 4-chlorokynurenine (AV-101), has been developed for use in humans, and is being studied in clinical trials as a potential treatment for major depressive disorder, and anti-nociception. In addition to antagonizing the NMDA receptor, 7-CKA also acts as a potent inhibitor of the reuptake of glutamate into synaptic vesicles (or as a vesicular glutamate reuptake inhibitor), an action that it mediates via competitive blockade of vesicular glutamate transporters (Ki = 0.59 mM). See also * 5,7-Dichlorokynurenic acid * Evans blue * Kynurenic acid * Xanthurenic acid Xanthurenic acid, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tool Compound
A tool is an object that can extend an individual's ability to modify features of the surrounding environment or help them accomplish a particular task. Although many animals use simple tools, only human beings, whose use of stone tools dates back hundreds of millennia, have been observed using tools to make other tools. Early human tools, made of such materials as stone, bone, and wood, were used for the preparation of food, hunting, the manufacture of weapons, and the working of materials to produce clothing and useful artifacts and crafts such as pottery, along with the construction of housing, businesses, infrastructure, and transportation. The development of metalworking made additional types of tools possible. Harnessing energy sources, such as animal power, wind, or steam, allowed increasingly complex tools to produce an even larger range of items, with the Industrial Revolution marking an inflection point in the use of tools. The introduction of widespread automation in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reagents For Biochemistry
In chemistry, a reagent ( ) or analytical reagent is a substance or compound added to a system to cause a chemical reaction, or test if one occurs. The terms ''reactant'' and ''reagent'' are often used interchangeably, but reactant specifies a substance ''consumed'' in the course of a chemical reaction. ''Solvents'', though involved in the reaction mechanism, are usually not called reactants. Similarly, ''catalysis, catalysts'' are not consumed by the reaction, so they are not reactants. In biochemistry, especially in connection with enzyme-catalyzed reactions, the reactants are commonly called substrate (biochemistry), substrates. Definitions Organic chemistry In organic chemistry, the term "reagent" denotes a chemical ingredient (a compound or mixture, typically of inorganic or small organic molecules) introduced to cause the desired transformation of an organic substance. Examples include the Collins reagent, Fenton's reagent, and Grignard reagents. Analytical chemistry ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Excitatory Amino Acid Reuptake Inhibitors
In neuroscience, an excitatory postsynaptic potential (EPSP) is a postsynaptic potential that makes the postsynaptic neuron more likely to fire an action potential. This temporary depolarization of postsynaptic membrane potential, caused by the flow of positively charged ions into the postsynaptic cell, is a result of opening ligand-gated ion channels. These are the opposite of inhibitory postsynaptic potentials (IPSPs), which usually result from the flow of ''negative'' ions into the cell or positive ions ''out'' of the cell. EPSPs can also result from a decrease in outgoing positive charges, while IPSPs are sometimes caused by an increase in positive charge outflow. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC). EPSPs, like IPSPs, are graded (i.e. they have an additive effect). When multiple EPSPs occur on a single patch of postsynaptic membrane, their combined effect is the sum of the individual EPSPs. Larger EPSPs result in greater membrane ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Quinolones
4-Quinolone is an organic compound derived from quinoline. It and 2-quinolone are the two most important parent (meaning simplified) quinolones. 4-Quinolone exists in equilibrium with a minor tautomer, 4-hydroxyquinoline (CAS#611-36-9). Aside from pedagogical interest, 4-quinolone is of little intrinsic value but its derivatives, the 4-quinolone antibiotics, represent a large class of important drugs. Synthesis The chemical synthesis of quinolones often involves ring-closing reactions.{{cite journal, title=Co(III)-Catalyzed Enaminone-Directed C-H Amidation for Quinolone Synthesis, author=Shi, Pengfei, author2=Wang, Lili, author3=Chen, Kehao, author4=Wang, Jie, author5=Zhu, Jin, journal= Organic Letters, year=2017, volume=19, issue=9, pages=2418–2421, pmid=28425721, doi=10.1021/acs.orglett.7b00968 Such reactions often install a hydroxyl group (an –OH functional group In organic chemistry, a functional group is any substituent or moiety (chemistry), moiety in a molecul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xanthurenic Acid
Xanthurenic acid, or xanthurenate, is a metabolic intermediate that accumulates and is excreted by pyridoxine (vitamin B6) deficient animals after the ingestion of tryptophan. Xanthurenic acid is suspected to be an endogenous agonist for Group II metabotropic glutamate receptors in humans. It is also known to be a potent VGLUT inhibitor, thereby preventing the movement of glutamate from the cytoplasm into synaptic vesicles, an action that it mediates via competitive blockade of vesicular glutamate transporters (Ki = 0.19 mM). researchers reported a marked reduction of xanthurenic acid levels in the serum of patients with schizophrenia. A recent meta-analysis showed that blood xanthurenic acid levels are lower in individuals suffering from bipolar disorder as well. Xanthurenic acid has also been shown to induce gametogenesis of ''Plasmodium falciparum'', the parasite that causes malaria. It is found in the gut of the ''Anopheles'' mosquito. See also * Kynurenic acid Kynure ... [...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] |
Evans Blue (dye)
T-1824 or Evans blue, often incorrectly rendered as Evan's blue, is an azo dye that has a very high affinity for serum albumin. Because of this, it can be useful in physiology in estimating the proportion of body water contained in blood plasma. It fluoresces with excitation peaks at 470 and 540 nm and an emission peak at 680 nm. Evans blue dye has been used as a viability assay on the basis of its penetration into non-viable cells, although the method is subject to error because it assumes that damaged or otherwise altered cells are not capable of repair and therefore are not viable. Evans blue is also used to assess the permeability of the blood–brain barrier to macromolecules. Because serum albumin cannot cross the barrier and virtually all Evans blue is bound to albumin, normally the neural tissue remains unstained. When the blood–brain barrier has been compromised, albumin-bound Evans blue enters the CNS. Evans blue is pharmacologically active, acting as a negat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5,7-Dichlorokynurenic Acid
5,7-Dichlorokynurenic acid (DCKA) is a selective NMDA receptor antagonist acting at the glycine site of the NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other ... complex.McNamara D, Smith EC, Calligaro DO, O'Malley PJ, McQuaid LA, Dingledine R. 5,7-Dichlorokynurenic acid, a potent and selective competitive antagonist of the glycine site on NMDA receptors. ''Neuroscience Letters''. 1990 Nov 27;120(1):17-20. See also * 7-Chlorokynurenic acid * Kynurenic acid References Enoic acids NMDA receptor antagonists Chloroarenes 4-Quinolones {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vesicular Glutamate Transporter
Vesicular glutamate transporter 1 (VGLUT1) is a protein that in humans is encoded by the ''SLC17A7'' gene. The protein encoded by this gene is a vesicle-bound, sodium-dependent phosphate transporter that is specifically expressed in the neuron-rich regions of the brain. It is preferentially associated with the membranes of synaptic vesicles and functions in glutamate transport. The protein shares 82% identity with the differentiation-associated Na-dependent inorganic phosphate cotransporter and they appear to form a distinct class within the Na+/Pi cotransporter family. See also * Solute carrier family The solute carrier (SLC) group of membrane transport proteins include over 400 members organized into 66 families. Most members of the SLC group are located in the cell membrane. The SLC gene nomenclature system was originally proposed by the HUGO ... References Further reading * * * * * * * * Solute carrier family Neurotransmitter transporters Glutamate (neurotransm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glutamate Reuptake Inhibitor
Glutamic acid (symbol Glu or E; known as glutamate in its anionic form) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can synthesize enough for its use. It is also the most abundant excitatory neurotransmitter in the vertebrate nervous system. It serves as the precursor for the synthesis of the inhibitory gamma-aminobutyric acid (GABA) in GABAergic neurons. Its molecular formula is . Glutamic acid exists in two optically isomeric forms; the dextrorotatory -form is usually obtained by hydrolysis of gluten or from the waste waters of beet-sugar manufacture or by fermentation.Webster's Third New International Dictionary of the English Language Unabridged, Third Edition, 1971. Its molecular structure could be idealized as HOOC−CH()−()2−COOH, with two carboxyl groups −COOH and one amino group −. However, in the solid state and mildly acidic water solution ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
