SML3526
AZD8529
≥98% (HPLC)
Synonym(s):
7-Methyl-5-(3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl)-2-(4-(trifluoromethoxy)benzyl)isoindolin-1-one, 7-Methyl-5-(3-piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one, AZD 8529
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About This Item
Empirical Formula (Hill Notation):
C24H24F3N5O3
CAS Number:
Molecular Weight:
487.47
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
AZD8529 is a selective metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator (PAM) that potentiates DCG-IV-induced GTPγS binding to membrane from human mGluR2, but not mGluR1/3/4/5/6/7/8, CaR/Gqi5 fusion-expressing HEK293 cells (EC50/Emax = 285 nM/59.9%) with no mGluR agonist/antagonist activity and little or no affinity toward a panel of 50 other receptors. AZD8529 is shown to reduce nicotine self-administration and cue-induced reinstatement of nicotine-seeking responses in squirrel monkeys (0.3-10 mg/kg i.m.) and rats (1.75-58.3 mg/kg) as well as cue-induced methamphetamine seeking in rats (20 and 40 mg/kg s.c.) in vivo.
Selective metabotropic glutamate receptor mGluR2 PAM with in vivo efficacy against self-administration & cue-induced reinstatement of substance seeking.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Zuzana Justinova et al.
Biological psychiatry, 78(7), 452-462 (2015-03-25)
Based on rodent studies, group II metabotropic glutamate receptors (mGluR2 and mGluR3) were suggested as targets for addiction treatment. However, LY379268 and other group II agonists do not discriminate between the mainly presynaptic inhibitory mGluR2 (the proposed treatment target) and
Xia Li et al.
Psychopharmacology, 233(10), 1801-1814 (2016-02-14)
Numerous medication development strategies seek to decrease nicotine consumption and prevent relapse to tobacco smoking by blocking glutamate transmission. Decreasing glutamate release by activating presynaptic inhibitory metabotropic glutamate (mGlu)2/3 receptors inhibits the reinforcing effects of nicotine and blocks cue-induced reinstatement
Daniel E O'Brien et al.
Molecular pharmacology, 93(5), 526-540 (2018-03-17)
Allosteric modulation of metabotropic glutamate receptor 2 (mGlu2) has demonstrated efficacy in preclinical rodent models of several brain disorders, leading to industry and academic drug discovery efforts. Although the pharmacology and binding sites of some mGlu2 allosteric modulators have been
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