AZD 2066 (hydrate)

386.33

10 mM in DMSO

GPCR/G Protein; Neuronal Signaling

AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects^[1]. IC50 & Target: mGluR5^[1] In Vitro: AZD 2066 (1-10 uM) 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 uM) 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 uM) has less e?ective in striatal neurons^[2]. In Vivo: AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in rats^[1].