Formulation: A crystalline solid
Formal Name: N-cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-3-pyridinecarboxamide, monohydrochloride
Purity: ≥98%
Formula Markup: C18H15FN2O • HCl
Formula Weight: 330,8
Shelf life (days): 1460
CAS Number: 1309976-62-2
Notes: VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} 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.{47576} 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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