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GRM4
Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the ''GRM4'' gene. Together with GRM6, GRM7 and GRM8 it belongs to Metabotropic glutamate receptor#Group II and Group III, group III of the metabotropic glutamate receptor family. Group III receptors are linked to the inhibition of the cyclic AMP cascade. Activation of GRM4 has potential therapeutic benefits in the treatment of parkinson's disease. Splice variant "taste-GRM4" is involved in the perception of umami taste. Ligands Orthosteric *Cinnabarinic acid, a tryptophan metabolite *LSP1-2111: agonist * LSP4-2022: agonist * LSP2-9166: mixed agonist at mGluR4 and mGluR7 Positive allosteric modulators (PAMs) * ADX88178 * Foliglurax (PXT-002331, DT-1687) * Tricyclic thiazolopyrazole derivative 22a: EC50 = 9 nM, Emax = 120% * ML-128: EC50 = 240 nM, Emax = 182% * Valiglurax (AP-472) (VU0652957) * VU-0418506 * VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift * VU0155041: subtype-selective PAM, intrinsi ... [...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 receptor, metabotropic process. They are members of the group C GPCR family, group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptor (biochemistry), 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 G protein-coupled receptor, seven transmembrane domains that span the cell membrane. Unlike ionotropic receptors, metabotropic glutamate receptors are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MGluR6
Glutamate receptor, metabotropic 6, also known as GRM6 or mGluR6, is a protein which in humans is encoded by the ''GRM6'' gene. 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 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 cyclic AMP cascade but differ in their agonist selectivities. mGluR6 is specifically expre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MGluR1
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. Alternativ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metabolic reactions, DNA replication, Cell signaling, responding to stimuli, providing Cytoskeleton, structure to cells and Fibrous protein, organisms, and Intracellular transport, transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the Nucleic acid sequence, nucleotide sequence of their genes, and which usually results in protein folding into a specific Protein structure, 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 pep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Foliglurax
Foliglurax (developmental code names PXT-002331, DT2331) is a positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4), which is under development by Prexton Therapeutics for the treatment of Parkinson's disease. It reached phase II clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...s, but while it was found to be safe and showed some signs of clinical improvement, it failed to sufficiently distinguish itself from placebo to meet the study endpoints. References Benzopyrans Experimental drugs MGlu4 receptor agonists 4-Morpholinyl compounds Nitroso compounds Thienopyridines {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PHCCC
PHCCC is a research drug which acts as a glutamate receptor ligand, particularly being a positive allosteric modulator at the mGluR4 subtype, as well as an agonist at mGluR6. It has anxiolytic effects in animal studies. PHCCC and similar drugs have been suggested as novel treatments for Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become .... See also * CPCCOEt References Cyclopropanes MGlu4 receptor agonists Ketoximes Anilides {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VU0155041
VU0155041 is an experimental drug that is a positive allosteric modulator for the glutamate receptor mGluR4. In animal studies it has anti-Parkinsonian action, reduces neuropathic pain such as allodynia, and counteracts the effects of opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ... addiction. References Experimental drugs Chlorobenzene derivatives Benzamides Carboxylic acids {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Valiglurax
Valiglurax (VU0652957) is an experimental drug that is a positive allosteric modulator for the glutamate receptor mGluR4. It was developed as a potential medication for the treatment of Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become .... References Experimental drugs Pyrazolopyridines Isoquinolines Trifluoromethyl compounds Secondary amines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ML-128
ML-1 was an experimental nuclear reactor built as part of the US Army Nuclear Power Program between 1961 and 1965. It was intended to provide truck-mounted nuclear power that could accompany troops from place to place and provide power to command and communication centers, evacuation hospitals, depots, and radar and weapons systems. Unlike the other seven reactors of this program, it did not use a steam turbine, but instead used a nitrogen coolant at to drive a closed-cycle gas turbine. It was designed to produce 3.3 MWthermal of heat and 400 kW of shaft horsepower with an outlet temperature of . Though the concept of a nitrogen closed cycle gas turbine was strong, the design failed to live up to expectations, and was abandoned with the closure of ML-1 in 1965 after several major refits and with only a few hundred hours of testing completed in all. Similar concepts have been more recently proposed as part of the PBMR program as derivatives thereof. A 1964 economic ana ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LSP2-9166
LSP2-9166 is a drug which acts as a selective agonist for the group III metabotropic glutamate receptors, with a reasonably potent EC50 of 70nM at mGluR4 and 220nM at mGluR7, and weaker activity of 1380nM at mGluR6 and 4800nM at mGluR8. It has anticonvulsant Anticonvulsants (also known as antiepileptic drugs, antiseizure drugs, or anti-seizure medications (ASM)) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also used in the treatme ... effects in animal studies, and reduces self-administration of various addictive drugs. References MGlu4 receptor agonists MGlu7 receptor agonists Trifluoromethyl ethers Dicarboxylic acids Alpha-Amino acids Phosphinates {{anticonvulsant-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
