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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). , Haldeman, B. -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.
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O'Hara PJ, Sheppard PO, Thogersen H, Venezia D, Haldeman BA, Mc Joly C, Gomeza J, Brabet I, Curry K, Bockaert J, Pin J-P. , Thomsen, C Joly, C. P.
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This module is connected to a heptahelical domain that activates G proteins.
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