VU0360172 (hydrochloride)

VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; K_i = 195 nM).¹ It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.² It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.

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1. Rodriguez, A.L., Grier, M.D., Jones, C.K., et al. Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol. Pharmacol. 78(6), 1105-1123 (2010).

2. Loane, D.J., Stoica, B.A., Tchantchou, F., et al. Novel mGluR5 positive allosteric modulator improves functional recovery, attenuates neurodegeneration, and alters microglial polarization after experimental traumatic brain injury. Neurotherapeutics 11(4), 857-869 (2014).