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LY-487,379
LY-487,379 is a drug used in scientific research that acts as a selective positive allosteric modulator for the metabotropic glutamate receptor group II subtype mGluR2. It is used to study the structure and function of this receptor subtype, and LY-487,379 along with various other mGluR2/3 agonists and positive modulators are being investigated as possible antipsychotic and anxiolytic drugs. See also * Eglumegad * HYDIA HYDIA is a drug that is used in neuroscience research, which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It has been useful in the mapping of the group II mGluR receptor proteins and the ... References Eli Lilly and Company brands MGlu2 receptor agonists MGlu3 receptor agonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 2
Metabotropic glutamate receptor 2 (mGluR2) is a protein that, in humans, is encoded by the ''GRM2'' gene. mGluR2 is a G protein-coupled receptor (GPCR) that couples with the Gi alpha subunit. The receptor functions as an autoreceptor for glutamate, that upon activation, inhibits the emptying of vesicular contents at the presynaptic terminal of glutamatergic neurons. Structure In humans, mGluR2 is encoded by the ''GRM2'' gene on chromosome 3. At least three protein-coding isoforms are predicted based on genomic information, as well as numerous non-coding isoforms. The mGluR2 protein is a seven-pass transmembrane protein. Function In humans, mGluR2 is only expressed in the brain, and not in any other tissue. In the brain, mGluR2 is expressed in neurons as well as astrocytes. Subcellularly, mGluR2 is predominantly positioned at the presynaptic terminal, although it is also expressed at the postsynaptic terminal. The metabotropic glutamate receptors are a family of G protein-co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Allosteric Modulation
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a Receptor (biochemistry), receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to (i.e., an ''allosteric site'') is not the same one to which an endogenous agonist of the receptor would bind (i.e., an ''orthosteric site''). Modulators and agonists can both be called receptor Ligand (biochemistry), ligands. Allosteric modulators can be 1 of 3 types either: positive, negative or neutral. Positive types increase the response of the receptor by increasing the probability that an agonist will bind to a receptor (i.e. Affinity (pharmacology), affinity), increasing its ability to activate the receptor (i.e. Efficacy (pharmacology), efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from binding to a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor
The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter. Function and structure The mGluRs perform a variety of functions in the central and peripheral nervous systems: For example, they are involved in learning, memory, anxiety, and the perception of pain. They are found in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, and the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Like other metabotropic receptors, mGluRs have seven transmembrane domains that span the cell membrane. Unlike ionotropic receptors, metabotropic glutamate receptors are not ion channels. Instead, they activate biochemical cascades, leading to the modification of o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotic
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eglumegad
Eglumetad (INN; also known as eglumegad) is a research drug developed by Eli Lilly and Company, which is being investigated for its potential in the treatment of anxiety and drug addiction. It is a glutamate derived compound and its mode of action implies a novel mechanism. Mechanism of action Eglumetad acts as a group-selective agonist for the group II metabotropic glutamate receptors ( mGluR2/ 3). It is unclear whether eglumetad directly interacts with dopamine D2 receptors. Effects In experiments on mice, eglumetad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment. Tests in humans confirmed that it produced anxiolytic effects without producing sedation. However it did slightly reduce cognitive performance in tests on monkeys. Eglumetad has also been found to be effective in relieving the symptoms of withdrawal from chro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HYDIA
HYDIA is a drug that is used in neuroscience research, which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It has been useful in the mapping of the group II mGluR receptor proteins and their molecular modeling. HYDIA is similar in structure to group II mGluR agonists such as eglumegad and LY-404,039, but the addition of the 3-hydroxy group reverses the activity to a competitive antagonist A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of r .... Other derivatives such as the 3-benzyloxy ether are more potent antagonists than HYDIA itself. References MGlu2 receptor antagonists MGlu3 receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eli Lilly And Company Brands
Eli most commonly refers to: * Eli (name), a given name, nickname and surname * Eli (biblical figure) Eli or ELI may also refer to: Film * ''Eli'' (2015 film), a Tamil film * ''Eli'' (2019 film), an American horror film Music * ''Eli'' (Jan Akkerman album) (1976) * ''Eli'' (Supernaut album) (2006) Places * Alni, Ardabil Province, Iran, also known as Elī * Eli, Mateh Binyamin, an Israeli settlement in the West Bank * Éile or Éli, a medieval kingdom in Ireland * Eli, Kentucky, United States * Eli, Nebraska, United States * Eli, West Virginia, United States Other uses * ''Eli'' (opera), an opera by Walter Steffens * ELI (programming language) * Earth Learning Idea * English language institute * Environmental Law Institute, an American environmental law policy organization * European Law Institute * European Legislation Identifier * Extreme Light Infrastructure, a proposed high energy laser research facility of the European Union * Eli, someone from Yale University, after ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
