| Bioactivity | AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes. | ||||||||||||
| Invitro | AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM[1].AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM[1]. | ||||||||||||
| In Vivo | AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1]. AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1]. Animal Model: | ||||||||||||
| Name | AZD-8529 | ||||||||||||
| CAS | 1092453-15-0 | ||||||||||||
| Formula | C24H24F3N5O3 | ||||||||||||
| Molar Mass | 487.47 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Justinova Z, et al. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62. |
AZD-8529
CAS: 1092453-15-0 F: C24H24F3N5O3 W: 487.47
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of
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