AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects.
IC50&Target
mGluR5
体外研究
AZD 2066 (1-10 μM) inhibits Ca 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.
AZD 2066 (1-10 μM) inhibits the oscillatory Ca response which induced by bath application of DHPG, and blocks either DHPG or Quis effects in mGlu5/HEK cells.
AZD 2066 (1-10 μM) has less effective in striatal neurons.
体内研究
AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in rats.
Animal Model:
Male Wistar rats (weighing 240-250 g)
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.
运输条件
Room temperature in continental US; may vary elsewhere.