298690-60-5

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). 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).

Ro 67-7476 is a positive allosteric metabotropic mGlu1 receptor modulator.

mGluR1a: 60.1 nM (EC₅₀)

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[1] F. KNOFLACH. Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site[J]. Proceedings of the National Academy of Sciences of the United States of America, 2001, 98 1: 13402-13407. DOI: 10.1073/pnas.231358298
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