Ro 01-6128

Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.¹ Ro 01-6128 is a positive allosteric modulator of mGluR1 that can potentiate glutamate-induced calcium release at rat mGluR1a with an EC₅₀ value of 104 nM.^2,3 Ro 01-6128 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate with an EC₅₀ value of 248 nM and potentiates glutamate-induced cAMP production with an EC₅₀ value of 21.5 μM.¹

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1. Sheffler, D.J., and Conn, P.J. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology 55(4), 419-427 (2008).

2. Knoflach, F., Mutel, V., Jolidon, S., et al. 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).

3. Hemstapat, K., de Paulis, T., Chen, Y., et al. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol. Pharmacol. 70(2), 616-626 (2006).