VU0361737

VU0361737 is a selective positive allosteric modulator (PAM) of mGluR4, displaying EC₅₀ values of 110 and 240 nM for rat and human receptors, respectively.¹ It has weak or no activity at other mGluRs.¹ VU0361737 passes the blood-brain barrier to act centrally in rats.^1,2 VU0361737, alone or in combination with an mGluR2 selective PAM, does not potentiate glutamate responses through mGlu2/4 heterodimers.³

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1. Engers, D.W., Niswender, C.M., Weaver, C.D., et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J. Med. Chem. 52(14), 4115-4118 (2009).

2. Engers, D.W., Field, J.R., Le, U., et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J. Med. Chem. 54(4), 1106-1110 (2011).

3. Kammermeier, P.J. Functional and pharmacological characteristics of metabotropic glutamate receptors 2/4 heterodimers. Mol. Pharmacol. 82(3), 438-447 (2012).