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AZD-8529 mesylate 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[1]. | [in vivo]
AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 mesylate (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1].
Animal Model: | Sprague-Dawley rats[1] | Dosage: | 10 mg/kg, 30 mg/kg | Administration: | Intraperitoneal injection; 2 hours before nicotine injections | Result: | Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats. |
| [IC 50]
mGluR2: 285 nM (EC50) | [References]
[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. DOI:10.1016/j.biopsych.2015.01.014 |
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