3-Pyridinecarboxamide, N-cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-

Biological Activity

VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[1].

References

[1]. Zuena AR, et al. In Vivo Non-radioactive Assessment of mGlu5 Receptor-Activated Polyphosphoinositide Hydrolysis in Response to Systemic Administration of a Positive Allosteric Modulator. Front Pharmacol. 2018 Jul 31;9:804.