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BAY is a potent (IC50 = μM) and selective antagonist at mGlu1 receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = μM). , McGrane, V. . Recently, the structure of the dimer of mGlu1 VFTMs revealed two important. , Thomsen, C Joly, C. M. J Neurosci.
This module is connected to a heptahelical domain that activates G proteins. () J. -P.
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Here, using molecular modeling and site-directed mutagenesis, we have identified residues in the GABAB1 subunit that are critical for agonist. , Brabet, I.
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