VU0409551

VU0409551 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 5 (mGluR5).¹ It induces calcium mobilization in HEK293 cells expressing human mGluR5 (EC₅₀ = 260 nM). It is selective for mGluR5 over mGluR1-4 and mGluR6-8 at 10 μM. VU0409551 reverses amphetamine-induced hyperlocomotion in rats (ED₅₀ = 23 mg/kg), indicating antipsychotic-like activity.¹ It increases levels of c-fos and expression of BDNF, Arc/Arg3.1, syntaxin 1A, and post-synaptic density-95 (PSD-95) in the hippocampus in the BACHD mouse model of Huntington's disease when administered at a dose of 3 mg/kg.² VU0409551 (3 mg/kg) also improves object location memory in the novel object location test and associative memory in the cued fear conditioning test in the BACHD mouse model.

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1. Conde-Ceide, S., Martínez-Viturro, C.M., Alcázar, J., et al. Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med. Chem. Lett. 6(6), 716-720 (2015).

2. Doria, J.G., de Souza, J.M., Silva, F.R., et al. The mGluR5 positive allosteric modulator VU0409551 improves synaptic plasticity and memory of a mouse model of Huntington’s disease. J. Neurochem. 147(2), 222-239 (2018).