Results 1 to 10 of about 25,145 (234)
Homology modelling of metabotropic glutamate receptor 2 [PDF]
Many studies show involvement of metabotropic glutamate receptors (mGluRs) in synaptic excitation transudation. The mGluR family consists of eight proteins divided into three groups corresponding to sequence similarities, pharmacology and physiological role. These groups are: I (mGluR1, -5), II (mGluR2, -3) and III (mGluR4, -6, -7, -8).
Mordalski S+4 more
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Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw+5 more
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Metabotropic glutamate receptor subtype 2 is a cellular receptor for rabies virus.
Rabies virus (RABV) invades the central nervous system and nearly always causes fatal disease in humans. How RABV interacts with host neuron membrane receptors to become internalized and cause rabid symptoms is not yet fully understood.
Jinliang Wang+12 more
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The C Terminus of the Metabotropic Glutamate Receptor Subtypes 2 and 7 Specifies the Receptor Signaling Pathways [PDF]
There is accumulating evidence that the specificity of the transduction cascades activated by G protein-coupled receptors cannot solely depend on the nature of the coupled G protein. To identify additional structural determinants, we studied two metabotropic glutamate (mGlu) receptors, the mGlu2 and mGlu7 receptors, that are both coupled to G(o ...
Julie Perroy+5 more
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Isolation-induced abnormal behaviors are useful animal models for assessing potential anti-psychotic drugs. This study examined the effect of MGS0028, a selective metabotropic glutamate 2/3 receptor agonist, on abnormal behaviors such as hyperactivity ...
Yukio Ago+10 more
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Functional and Pharmacological Characteristics of Metabotropic Glutamate Receptors 2/4 Heterodimers [PDF]
Metabotropic glutamate receptors (mGluRs) were thought until recently to function mainly as stable homodimers, but recent work suggests that heteromerization is possible. Despite the growth in available compounds targeting mGluRs, little is known about the pharmacological profile of mGluR heterodimers. Here, this question was addressed for the mGluR2/4
Paul J. Kammermeier
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AbstractAntidepressant drugs have a clinical latency that correlates with the development of neuroadaptive changes, including down‐regulation of β‐adrenergic receptors in different brain regions. The identification of drugs that shorten this latency will have a great impact on the treatment of major depressive disorders.
Francesco Matrisciano+11 more
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Elevated level of metabotropic glutamate receptor 2/3 in the prefrontal cortex in major depression [PDF]
Clinical, postmortem and preclinical research strongly implicates dysregulation of glutamatergic neurotransmission in major depressive disorder (MDD). Recently, metabotropic glutamate receptors (mGluRs) have been proposed as attractive targets for the discovery of novel therapeutic approaches against depression.
Anteneh M. Feyissa+8 more
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Alcohol abuse is a leading risk factor for the public health burden worldwide. Approved pharmacotherapies have demonstrated limited effectiveness over the last few decades in treating alcohol use disorders (AUD).
Kevin Domanegg+2 more
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Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization [PDF]
Covalent labeling of G protein-coupled receptors (GPCRs) by small molecules is a powerful approach to understand binding modes, mechanism of action, pharmacology, and even facilitate structure elucidation. We report the first covalent positive allosteric modulator (PAM) for a class C GPCR, the mGlu2 receptor.
Maarten L. J. Doornbos+10 more
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