Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu 5 negative allosteric modulation
نویسندگان
چکیده
منابع مشابه
Neurobiological Insights from mGlu Receptor Allosteric Modulation
Allosteric modulation of metabotropic glutamate (mGlu) receptors offers a promising pharmacological approach to normalize neural circuit dysfunction associated with various psychiatric and neurological disorders. As mGlu receptor allosteric modulators progress through discovery and clinical development, both technical advances and novel tool compounds are providing opportunities to better under...
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The metabotropic glutamate receptor family comprises eight subtypes (mGlu1-8) of G-protein coupled receptors. mGlu receptors have a large extracellular domain which acts as recognition domain for the natural agonist glutamate. In contrast to the ionotropic glutamate receptors which mediate the fast excitatory neurotransmission, mGlu receptors have been shown to play a more modulatory role and h...
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Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGlu5) have potential applications in the treatment of fragile X syndrome, levodopa-induced dyskinesia in Parkinson disease, Alzheimer disease, addiction, and anxiety; however, clinical and preclinical studies raise concerns that complete blockade of mGlu5 and inverse agonist activity of current mGlu5 NAMs contr...
متن کاملPartial negative allosteric modulator of the subtype 5 metabotropic glutamate receptor with in vivo efficacy
Affiliations: Department of Pathology, Microbiology and Immunology, Division of Neuropathology (H.H.N., J.P.Y.); Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery (H.H.N., R.D.M., B.S.B., K.A.E., M.B., W.P., M.T.N., A.T., X.L., Z.X., J.S.D., C.M.N., C.W.L., C.K.J., P.J.C.); Department of Chemistry and Vanderbilt Institute of Chemical Biology (S.R.S., K.A.E., C.W.L...
متن کاملPositive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine
We investigated the role of metabotropic glutamate receptor type 5 (mGluR5) in methamphetamine-induced behavioral sensitization. The mGluR5 positive allosteric modulator (3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamide (CDPPB) and negative allosteric modulator fenobam were tested in separate experiments. Sprague-Dawley rats were repeatedly injected with 1 mg/kg methamphetamine or saline, and...
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2017
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2017.01.013