| Identification | Back Directory | [Name]
7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one | [CAS]
1092453-15-0 | [Synonyms]
AZD-8529
AZD 8529,AZD8529
AZD-8529 free base
1H-Isoindol-1-one, 2,3-dihydro-7-methyl-5-[3-(1-piperazinylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-
7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one | [EINECS(EC#)]
680-652-6 | [Molecular Formula]
C24H24F3N5O3 | [MDL Number]
MFCD31657360 | [MOL File]
1092453-15-0.mol | [Molecular Weight]
487.47 |
| Chemical Properties | Back Directory | [Boiling point ]
650.9±65.0 °C(Predicted) | [density ]
1.361±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:62.5(Max Conc. mg/mL);128.21(Max Conc. mM) | [form ]
Oil | [pka]
8.79±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
AZD8529 is a selective metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator (PAM) th at potentiates DCG-IV-induced GTPγS binding to membrane from human mGluR2but not mGluR1/3/4/5/6/7/8CaR/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. | [in vivo]
AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 (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) | [storage]
Store at -20°C | [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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| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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