AZD 2066 hydrate 

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 effects in mGlu5/HEK cells^[2].
AZD 2066 (1-10 μM) has less effective in striatal neurons^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

386.33

C₁₉H₁₆ClN₅O₂.1/4H₂O

Solid

Off-white to light yellow

CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C.O.[1/4]

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]