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Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).1 It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).2
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1. Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site. Proc. Natl. Acad. Sci. USA 98(23), 13402-13407 (2001).
2. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology 55(4), 419-427 (2008).