Metabotropic Glutamate Receptor 2
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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-cou ...
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Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, responding to stimuli, providing structure to cells and organisms, and transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the nucleotide sequence of their genes, and which usually results in protein folding into a specific 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called peptides. The individual amino acid residues are bonded together by peptide bonds and adjacent amino acid residues. The sequence of amino acid ...
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GPCR Oligomer
A GPCR oligomer is a protein complex that consists of a small number ( ''oligoi'' "a few", ''méros'' "part, piece, component") of G protein-coupled receptors (GPCRs). It is held together by covalent bonds or by intermolecular forces. The subunits within this complex are called protomers, while unconnected receptors are called monomers. Receptor homomers consist of identical protomers, while heteromers consist of different protomers. Receptor homodimers – which consist of two identical GPCRs – are the simplest homomeric GPCR oligomers. Receptor heterodimers – which consist of two different GPCRs – are the simplest heteromeric GPCR oligomers. The existence of receptor oligomers is a general phenomenon, whose discovery has superseded the prevailing paradigmatic concept of the function of receptors as plain monomers, and has far-reaching implications for the understanding of neurobiological diseases as well as for the development of drugs. Discovery For a long time ...
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Psychedelic Drug
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary states of consciousness (known as psychedelic experiences or "trips").Pollan, Michael (2018). ''How to Change Your Mind: What the New Science of Psychedelics Teaches Us About Consciousness, Dying, Addiction, Depression, and Transcendence'' Sometimes, they are called classic hallucinogens, serotonergic hallucinogens, or serotonergic psychedelics, and the term ''psychedelics'' is used more broadly to include all hallucinogens; this article uses the narrower definition of ''psychedelics''. Psychedelics cause specific psychological, visual, and auditory changes, and often a substantially altered state of consciousness.Leary, Timothy; Metzner, Ralph (1964). ''The Psychedelic Experience: A Manual Based on The Tibetan Book of the Dead'' Psychedelic states are often compared to meditative, psychodynamic or transcendental types of alterations of mind. The "classical" psychedelics, the ...
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RO4491533
RO-4491533 is a drug developed by Hoffmann-La Roche which acts as a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors ( mGluR2/3), being equipotent at mGluR2 and mGluR3 but without activity at other mGluR subtypes. In animal studies, RO-4491533 produced antidepressant effects and reversed the effects of the mGluR2/3 agonist LY-379,268 with similar efficacy but slightly lower potency than the mGluR2/3 antagonist LY-341,495. A number of related compounds are known, with similar effects ''in vitro'' and a fairly well characterized structure-activity relationship. See also * Decoglurant Decoglurant ( INN) (code name RG1578, RO4995819) is a negative allosteric modulator of the mGlu2 and mGlu3 receptors which was under development by Roche for the adjunctive treatment of major depressive disorder. Decoglurant progressed as far ... References MGlu2 receptor antagonists MGlu3 receptor antagonists Trifluorome ...
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EGLU
EGLU ((2S)-α-ethylglutamic acid ) is a drug that is used in neuroscience research. It was one of the first compounds found that acts as a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), and so has been useful in the characterization and study of this receptor subfamily. References MGlu2 receptor antagonists MGlu3 receptor antagonists Amino acids Dicarboxylic acids {{nervous-system-drug-stub ...
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MGS-0039
MGS-0039 is a drug that is used in neuroscientific research, which acts as a potent and selective antagonist for group II of the metabotropic glutamate receptors ( mGluR2/3). It produces antidepressant and anxiolytic effects in animal studies, and has been shown to boost release of dopamine and serotonin in specific brain areas. Research has suggested this may occur through a similar mechanism as that suggested for the similarly glutamatergic drug ketamine Ketamine is a dissociative anesthetic used medically for induction and maintenance of anesthesia. It is also used as a recreational drug. It is one of the safest anesthetics, as, in contrast with opiates, ether, and propofol, it suppress .... References {{Metabotropic glutamate receptor modulators MGlu2 receptor antagonists MGlu3 receptor antagonists ...
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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 several different areas, showing antidepressant effects in animal models, increasing the behavioural effects of hallucinogenic drugs in animal tests, and increasing the analgesic effects of μ-opioid agonists, as well as modulating dopamine receptor function. The 1-fluorocyclopropane analog has a superior pharmacokinetic profile and similar mGluR2/3 affinity, and making a prodrug from this with the heptyl ester increases bioavailability still further. See also * CECXG CECXG (3'-ethyl-LY-341,495) is a research drug which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors ( mGluR2/3), with reasonable selectivity for mGluR3. While it is some five times less potent than LY ... References ...
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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 ...
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Biphenylindanone A
Biphenylindanone A (BINA, LS-193,571) is a research agent which acts as a potent and selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2. In animal studies it showed anxiolytic and antipsychotic effects, and blocked the effects produced by the hallucinogenic drug DOB. BINA and other selective mGluR2 positive modulators have therefore been suggested as a novel class of drugs for the treatment of schizophrenia which may have superior properties to traditional antipsychotic drugs. BINA decreases cocaine self-administration in rats, with no effect on food self-administration, and is in regard to this discrimination superior to the mGluR2/3 agonist LY-379,268 LY-379,268 is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is derived from the older mGluR group II agonist eglumegad, and led on to .... References An ...
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JNJ-40411813
ADX-71149, also known as JNJ-40411813 and JNJ-mGluR2-PAM, is a selective positive allosteric modulator of the mGlu2 receptor. It is being studied by Addex Therapeutics and Janssen Pharmaceuticals for the treatment of schizophrenia. It was also researched by these companies for the treatment of anxious depression (major depressive disorder with anxiety symptoms), but although some efficacy was observed in clinical trials, it was not enough to warrant further development for this indication. , ADX-71149 is in phase II clinical trials for schizophrenia. See also * Biphenylindanone A * Eglumegad * LY-404,039 * LY-379,268 LY-379,268 is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is derived from the older mGluR group II agonist eglumegad, and led on to ... * LY-487,379 References External links ADX71149 for Schizophrenia - Addex TherapeuticsADX71149 for A ...
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Dhanya 2010
Dhanya may refer to: * ''Dhanya'' (film), a 1981 Indian Malayalam film * ''Dhanya'' (beetle), a genus of beetles in the family Carabidae * Dhanya is the Sanskrit word for gratitude People * Dhanya Balakrishna, Indian actress * Dhanya Manikya (died 1515), Maharaja of Tripura from 1463 * Dhanya Mary Varghese Dhanya Mary Varghese is an Indian actress known for her work in the Malayalam cinema and television. She has appeared in over 20 films, the majority of which were in Malayalam. Aside from movies, she has appeared in a number of television show ...
(born 1985), Indian actress {{Disambiguation ...
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