AZD 2066 

AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 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].

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

AZD 2066 (0.3-30 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.

381.82

C₁₉H₁₆ClN₅O₂

934282-55-0

Solid

White to off-white

CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Swedberg MD, 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]