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SML3526

Sigma-Aldrich

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:
1092453-15-0
Molecular Weight:
487.47
MDL number:
MFCD31657360
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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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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