Abstract：
:The metabotropic glutamate (mGlu) receptors are a family of G-protein-coupled receptors (GPCRs) that regulate cell physiology throughout the nervous system. The potential of mGlu receptors as therapeutic targets has been bolstered by current research that has provided insight into the diverse modes of mGlu activation and signaling. In particular, the allosteric modulation of mGlu receptors represents a major area of focus in studies of basic pharmacology as well as drug development, largely due to the high subtype specificity achievable by targeting allosteric sites on mGlu receptors. These provide sophisticated regulation of neuronal excitability and synaptic transmission to influence behavioral output. Here, we review how these allosteric mechanisms have been leveraged preclinically to demonstrate the therapeutic potential of allosteric modulators for neurological and neuropsychiatric disorders, such as autism, cognitive impairment, Parkinson's disease (PD), stress, and schizophrenia.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Stansley BJ,Conn PJdoi
10.1016/j.tips.2019.02.006subject
Has Abstractpub_date
2019-04-01 00:00:00pages
240-252issue
4eissn
0165-6147issn
1873-3735pii
S0165-6147(19)30037-9journal_volume
40pub_type
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