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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 Kynurenic acid (KYNA or KYN) is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tool Compound
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, ''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 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 In analytical chemistry, a reage ... [...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, ... [...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, ''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 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 In analytical chemistry, a reagen ... [...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) on the carbon across from the ring nitrogen (i.e., the C-4 positions). An example of such a synthesis is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xanthurenic Acid
Xanthurenic acid, or xanthurenate, is a chemical shown to induce gametogenesis of '' Plasmodium falciparum'', the parasite that causes malaria. It is found in the gut of the ''Anopheles'' mosquito. Xanthurenic acid 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. See also * Kynurenic acid Kynu ... [...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 neg ... [...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 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 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 ... 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 Cotransporters are a subcategory of membrane transport proteins (transporters) that couple the favorable movement of one molecule with its concentration gradient and unfavorable movement of another molecule against its concentration gradient. They e ... family. See also * Solute carrier family References Further reading * * * * * * * * Solute carrier family Neurotransmitter transporters Glutamate (neurotrans ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glutamate Reuptake Inhibitor
An excitatory amino acid reuptake inhibitor (EAARI) is a type of drug which inhibits the reuptake of the excitatory neurotransmitters glutamate and aspartate by blocking one or more of the excitatory amino acid transporters (EAATs). Examples of EAARIs include dihydrokainic acid (DHK) and WAY-213,613, selective blockers of EAAT2 (GLT-1), and L-''trans''-2,4-PDC, a non-selective blocker of all five EAATs. Amphetamine is a selective noncompetitive reuptake inhibitor of presynaptic EAAT3 (via transporter endocytosis) in dopamine neurons. L-Theanine is reported to competitively inhibit reuptake at EAAT1 (GLAST) and EAAT2 (GLT-1). See also * Reuptake inhibitor * Glutamatergic * GABA reuptake inhibitor * Glycine reuptake inhibitor * Excitatory amino acid receptor agonist * Excitatory amino acid receptor antagonist An excitatory amino acid receptor antagonist, or glutamate receptor antagonist, is a chemical substance which Receptor antagonist, antagonizes one or more of the glutamate rec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
