AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects[1].
AZD 2066 (1-10 μM) inhibits Ca2+ response, with IC50s 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 Ca2+ 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]
[1]. Swedberg MDB, et, al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug; 350(2): 212-22. [2]. Jong YJI, et, al. Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu 5, Negative Allosteric Modulators. ACS Chem Neurosci. 2019 Nov 20; 10(11): 4558-4570.