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MGluR5
Metabotropic glutamate receptor 5 is an excitatory Gq-coupled G protein-coupled receptor predominantly expressed on the postsynaptic sites of neurons. In humans, it is encoded by the ''GRM5'' gene. Function The amino acid L- glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacological properties. Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7, and GRM8. Group II and III receptors are linked to the inhibition of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mavoglurant
Mavoglurant (developmental code name AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome and other conditions which has been discontinued. It exerts its effect as an receptor antagonist, antagonist of the metabotropic glutamate receptor 5 (mGluR5). Mavoglurant was under drug development, development by Novartis and reached phase II and phase III clinical trials. Phase IIb/III dose finding and evaluation trials for fragile X-syndrome were discontinued by the end of 2014. Otherwise, it would have been the first drug to treat the underlying disorder instead of the symptoms of fragile X syndrome. Mavoglurant was also in phase II clinical trials for Levodopa-induced dyskinesia. In 2007, Norvartis had conducted a clinical study to assess its ability of reducing cigarette smoking, but no results had been published up till now. Novartis was conducting a clinical trial with this drug on obsessive–compulsive disorder. Novartis discontinued development of ma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 1
The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein. Function L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group I, which includes GRM1 alongside GRM5, have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Alternative s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 3
Metabotropic glutamate receptor 3 (mGluR3) is an inhibitory Gi/G0-coupled G-protein coupled receptor (GPCR) generally localized to presynaptic sites of neurons in classical circuits. However, in higher cortical circuits in primates, mGluR3 are localized post-synaptically, where they strengthen rather than weaken synaptic connectivity. In humans, mGluR3 is encoded by the ''GRM3'' gene. Deficits in mGluR3 signaling have been linked to impaired cognition in humans, and to increased risk of schizophrenia, consistent with their expanding role in cortical evolution. Structure In humans, mGluR3 is encoded by the GRM3 gene on chromosome 7. At least five protein-coding isoforms are predicted based on genomic information. The mGluR3 protein is a seven-pass transmembrane protein. Function L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gq Alpha Subunit
Gq protein alpha subunit is a family of heterotrimeric G protein alpha subunits. This family is also commonly called the Gq/11 (Gq/G11) family or Gq/11/14/15 family to include closely related family members. G alpha subunits may be referred to as Gq alpha, Gαq, or Gqα. Gq proteins couple to G protein-coupled receptors to activate beta-type phospholipase C (PLC-β) enzymes. PLC-β in turn hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP2) to diacyl glycerol (DAG) and inositol trisphosphate (IP3). IP3 acts as a second messenger to release stored calcium into the cytoplasm, while DAG acts as a second messenger that activates protein kinase C (PKC). Family members In humans, there are four distinct proteins in the Gq alpha subunit family: * Gαq is encoded by the gene GNAQ. * Gα11 is encoded by the gene GNA11. * Gα14 is encoded by the gene GNA14. * Gα15 is encoded by the gene GNA15. Function The general function of Gq is to activate intracellular signaling p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CAMP-dependent Pathway
In the field of molecular biology, the cAMP-dependent pathway, also known as the adenylyl cyclase pathway, is a G protein-coupled receptor-triggered signaling cascade used in cell communication. Discovery cAMP was discovered by Earl Sutherland and Ted Rall. cAMP is considered a secondary messenger along with Ca2+. Sutherland won the Nobel Prize in 1971 for his discovery of the mechanism of action of epinephrine in glycogenolysis, that requires cAMP as secondary messenger. Mechanism G protein-coupled receptors (GPCRs) are a large family of integral membrane proteins that respond to a variety of extracellular stimuli. Each GPCR binds to and is activated by a specific ligand stimulus that ranges in size from small molecule catecholamines, lipids, or neurotransmitters to large protein hormones. When a GPCR is activated by its extracellular ligand, a conformational change is induced in the receptor that is transmitted to an attached intracellular heterotrimeric G protein complex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Remeglurant
Remeglurant (; developmental code name MRZ-8456) is a drug which acts as a selective antagonist of the mGlu5 receptor. It is under development by Merz Pharmaceuticals for the treatment of drug-induced dyskinesia but no development has been reported since at least 2016. See also * Basimglurant * Dipraglurant * Fenobam * Mavoglurant * Raseglurant Raseglurant (INN) (code name ADX-10059) is a negative allosteric modulator of the mGlu5 receptor and derivative of MPEP which was under development by Addex Therapeutics for the treatment of migraine, gastroesophageal reflux disease, and denta ... References Isoquinolines MGlu5 receptor antagonists Organobromides Pyrimidines {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-344,545
LY-344,545 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as an antagonist for the metabotropic glutamate receptor subtype mGluR5. It is an epimer of another metabotropic glutamate receptor antagonist, the mGluR2/3-selective LY-341,495 LY-341495 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as a potent and selective orthosteric antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is used in scientific research in severa .... References Eli Lilly and Company brands MGlu5 receptor antagonists Xanthenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lithium (medication)
Certain lithium compounds, also known as lithium salts, are used as psychiatric medication, primarily for bipolar disorder and for major depressive disorder. In these disorders, it sometimes reduces the risk of suicide. Lithium is taken orally. Common side effects include increased urination, shakiness of the hands, and increased thirst. Serious side effects include hypothyroidism, diabetes insipidus, and lithium toxicity. Blood level monitoring is recommended to decrease the risk of potential toxicity. If levels become too high, diarrhea, vomiting, poor coordination, sleepiness, and ringing in the ears may occur. Lithium is teratogenic, especially during the first trimester of pregnancy and at higher dosages. The use of lithium while breastfeeding is controversial; however, many international health authorities advise against it, and the long-term outcomes of perinatal lithium exposure have not been studied. The American Academy of Pediatrics lists lithium as contraindicat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glutamate
Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) 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 GABA-ergic neurons. Its molecular formula is . Glutamic acid exists in three 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 solu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monellin
Monellin, a sweet protein, was discovered in 1969 in the fruit of the West African shrub known as serendipity berry (''Dioscoreophyllum cumminsii''); it was first reported as a carbohydrate.GE Inglett, JF May. Serendipity berries - Source of a new intense sweetener. J Food Sci 1969, 34:408-411. The protein was named in 1972 after the Monell Chemical Senses Center in Philadelphia, U.S.A., where it was isolated and characterized. Protein composition Monellin's molecular weight is 10.7 Atomic mass unit, kDa. It has two noncovalently associated polypeptide chains: an A chain sequence with 44 amino acid residues, and a B chain with 50 residues. Monellin chain A (44 AA): Monellin chain B (50 AA): Amino acid#Table of standard amino acid abbreviations and properties, Amino acid sequence of the sweet protein monellin adapted from Swiss-Prot biological database of protein. Monellin has a secondary structure consisting of five beta-strands that form an antiparallel beta-sheet and a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nootropic
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the ethics and fairness of their use, concerns over adverse effects, and the diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at a CAGR of 14.8%. While most nootropics are not regulated, there are ot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Radiotracer
A radioactive tracer, radiotracer, or radioactive label is a chemical compound in which one or more atoms have been replaced by a radionuclide so by virtue of its radioactive decay it can be used to explore the mechanism of chemical reactions by tracing the path that the radioisotope follows from reactants to products. Radiolabeling or radiotracing is thus the radioactive form of isotopic labeling. In biological contexts, use of radioisotope tracers are sometimes called radioisotope feeding experiments. Radioisotopes of hydrogen, carbon, phosphorus, sulfur, and iodine have been used extensively to trace the path of biochemical reactions. A radioactive tracer can also be used to track the distribution of a substance within a natural system such as a cell or tissue, or as a flow tracer to track fluid flow. Radioactive tracers are also used to determine the location of fractures created by hydraulic fracturing in natural gas production.Reis, John C. (1976). ''Environmental Control in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
