| Bioactivity | AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 has antinociception effects[1]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | AZD 2066 (0.3-30 mg/kg; p.o.) shows discriminative effects in rats[1]. Animal Model: | ||||||||||||
| Name | AZD 2066 | ||||||||||||
| CAS | 934282-55-0 | ||||||||||||
| Formula | C19H16ClN5O2 | ||||||||||||
| Molar Mass | 381.82 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |