Cas No.: | 1092453-15-0 |
Chemical Name: | AZD-8529 free base |
Synonyms: | AZD 8529;AZD-8529;AZD8529 |
SMILES: | CC1=CC(=CC2=C1C(=O)N(C2)CC3=CC=C(C=C3)OC(F)(F)F)C4=NC(=NO4)CN5CCNCC5 |
Formula: | C24H24F3N5O3 |
M.Wt: | 487.483 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |
Target: | EC50: 285 nM (mGluR2)[1] |
In Vivo: | AZD-8529 (0.3, 1 or 3 mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys. AZD-8529 (30 mg/kg) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1]. |
In Vitro: | 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. AZD8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195±62 nM[1]. |
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. |