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

AZD 2066 (1-10 μM) inhibits Ca 2+ response, with IC 50 s of 27.2±9.1, 3.56±0.52, 96.2±17.8, and 380±78.0 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively [2]. AZD 2066 (1-10 μM) inhibits the oscillatory Ca 2+ response which induced by bath application of DHPG, and blocks either DHPG or Quis e ects in mGlu5/HEK cells [2]. AZD 2066 (1-10 μM) has less e ective in striatal neurons [2].

AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in rats [1]. Animal Model: Male Wistar rats (weighing 240-250 g) [1] Dosage: 0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg Administration: P.o. (60 minutes after administration) Result: Caused full and dose-dependent AZD9272-appropriate responding.