AZD 2066 hydrate is a selective, orally active, brain-penetrant mGluR5 antagonist with antinociceptive effects [1].

AZD 2066, at concentrations ranging from 1-10 μM, effectively inhibits the Ca2+ response, demonstrating IC50 values of 27.2±9.1 nM in mGlu5/HEK cells, 3.56±0.52 nM in striatal cultures, 96.2±17.8 nM in hippocampal cultures, and 380±78.0 nM in cortical cultures. Additionally, this compound suppresses the oscillatory Ca2+ response induced by DHPG and blocks the effects of either DHPG or Quis in mGlu5/HEK cells. However, it is less effective in striatal neurons.

AZD 2066 (0.03-30 mg/kg; p.o.) exhibits dose-dependent discriminative effects in 240-250g male Wistar rats, producing a complete and dose-proportional response specific to AZD9272 60 minutes post-administration, demonstrating its activity at various dosages [1].