Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators
نویسندگان
چکیده
منابع مشابه
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
Allosteric modulators of G protein-coupled receptors (GPCRs) have a number of potential advantages compared to agonists or antagonists that bind to the orthosteric site of the receptor. These include the potential for receptor selectivity, maintenance of the temporal and spatial fidelity of signaling in vivo, the ceiling effect of the allosteric cooperativity which may prevent overdose issues, ...
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Although relatively few G-protein-coupled receptors are Class C, in recent years, this small family of receptors has become a focal point for the discovery of new and exciting allosteric modulators. The mGlu (metabotropic glutamate) receptors are illustrative in the discovery of both positive and/or negative allosteric modulators with unique pharmacological properties. For instance, allosteric ...
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μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential. Efforts to fine tune pain control while alleviating the s...
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The receptor for TSH (TSHR) has captured our interest and imagination since it was first demonstrated to be a major human antigen in autoimmune thyroid disease. The original realization that the immunoglobulin fraction of sera from patients with Graves’ disease incorporated unique human autoantibodies to the TSHR led to the unraveling of the great complexity that the TSHR exhibits in comparison...
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ژورنال
عنوان ژورنال: Molecular Pharmacology
سال: 2018
ISSN: 0026-895X,1521-0111
DOI: 10.1124/mol.117.110114