AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG -stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain.
AZD6538 completely reverses the glutamate-stimulated (EC80, 80 μM) phosphatidyl inositol drolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with an IC50 of 51 ± 3 nM[1].
References:
[1]. Raboisson P, et al. Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6974-9.