For research use only. Not for therapeutic Use.
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 effects in mGlu5/HEK cells[2].
AZD 2066 (1-10 μM) has less effective in striatal neurons[2].
AZD 2066 (0.3-30 mg/kg; p.o.) shows discriminative effects in rats[1].
Catalog Number | I011256 |
CAS Number | 934282-55-0 |
Synonyms | 5-(3-chlorophenyl)-3-[(1R)-1-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)oxy]ethyl]-1,2-oxazole |
Molecular Formula | C19H16ClN5O2 |
Purity | ≥95% |
InChI | InChI=1S/C19H16ClN5O2/c1-12(16-11-17(27-24-16)14-4-3-5-15(20)10-14)26-19-23-22-18(25(19)2)13-6-8-21-9-7-13/h3-12H,1-2H3/t12-/m1/s1 |
InChIKey | SXWHYTICXCLKDG-GFCCVEGCSA-N |
SMILES | CC(C1=NOC(=C1)C2=CC(=CC=C2)Cl)OC3=NN=C(N3C)C4=CC=NC=C4 |
Reference | [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. [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. |