General paperPhenylglycine derivatives discriminate between mGluR1- and mGluR5-mediated responses
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Symmetric signal transduction and negative allosteric modulation of heterodimeric mGlu1/5 receptors
2021, NeuropharmacologyCitation Excerpt :This indicates that heterodimers assembled from transfected mGlu1F781S and endogenous mGlu5 have a reduced signaling efficiency in response to DHPG compared to the endogenous mGlu5 homodimers. This is in line with experiments in transfected HEK293 cells (Fig. 7D) and likely relates to the reduced potency of DHPG at mGlu1 compared to mGlu5 (Brabet et al., 1995; Lin et al., 1997). Time-resolved FRET experiments showed that mGluRs assemble heteromeric receptors in heterologous cells (Doumazane et al., 2011).
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2016, NeuroscienceMetabotropic glutamate receptors are involved in the detection of IMP and L-amino acids by mouse taste sensory cells
2016, NeuroscienceCitation Excerpt :We used selective agonists and antagonists to investigate the role of group I mGluRs in detection of l-amino acids and IMP. For an mGluR1 agonist, we used DHPG, an orthosteric agonist for group I mGluRs with similar potencies at mGluR1 and mGluR5 (Brabet et al., 1995; Wisniewski and Car, 2002). At low concentrations, DHPG is highly selective for group I mGluRs.
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2015, Bioorganic and Medicinal Chemistry LettersThe role of intracellular calcium stores in synaptic plasticity and memory consolidation
2013, Neuroscience and Biobehavioral ReviewsCitation Excerpt :However, specific inhibition of the mGluR5 subtype using MPEP (8 mM, administered immediately post-training) or the competitive mGluR1 antagonist LY 367385 (7.5 nmol/hemisphere, administered 5 min prior to training) impaired retention from 15 min post-training using a non-discriminant variant of the same task (Gieros et al., 2012; Salinska, 2006). A possible explanation for this inconsistency is that MCPG is regarded as somewhat of an irregular group I antagonist (Huber et al., 1998; Schoepp et al., 1999) by having more potency for antagonising mGluR1 than mGluR5 (Brabet et al., 1995; Kingston et al., 1995). Therefore, MCPG may not have been sufficiently potent to antagonise mGluR5 or mGluR1 and disrupt memory at 15 min post-training.