AZD-8529 mesylate

• CAT Number: I016691
• CAS Number: 1314217-69-0
• Molecular Formula: C25H28F3N5O6S
• Molecular Weight: 583.58
• Purity: ≥95%
• Synonyms: methanesulfonic acid;7-methyl-5-[3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-3H-isoindol-1-one
• InChI: InChI=1S/C24H24F3N5O3.CH4O3S/c1-15-10-17(22-29-20(30-35-22)14-31-8-6-28-7-9-31)11-18-13-32(23(33)21(15)18)12-16-2-4-19(5-3-16)34-24(25,26)27;1-5(2,3)4/h2-5,10-11,28H,6-9,12-14H2,1H3;1H3,(H,2,3,4)
• InChIKey: HRHCPVNKPOTCGB-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC2=C1C(=O)N(C2)CC3=CC=C(C=C3)OC(F)(F)F)C4=NC(=NO4)CN5CCNCC5.CS(=O)(=O)O

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].
AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM [1].
AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM[1].
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].

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.
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