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首页-小分子抑制剂&激动剂-GPCR-mGluR-AZD8529
AZD8529

Chemical Structure : AZD8529

CAS No.: 1092453-15-0

AZD8529 (AZD-8529)

货号: PC-63180Not For Human Use, Lab Use Only.

AZD8529 (AZD-8529) is a novel potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD8529 (AZD-8529) is a novel potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes.
AZD8529 potentiates agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus and striatum.
AZD8529 decreases nicotine self-administration at doses (0.3-3 mg/kg) in monkeys, also reduces nicotine priming- and cue-induced reinstatement of nicotine seeking, decreases nicotine-induced accumbens dopamine release in rats.

物理化学性质&存储条件

分子量 487.483
分子式 C24H24F3N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,3-Dihydro-7-methyl-5-[3-(1-piperazinylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-1H-isoindol-1-one

参考文献

1. Justinova Z, et al. Biol Psychiatry. 2015 Oct 1;78(7):452-62.

2. Caprioli D, et al. Biol Psychiatry. 2015 Oct 1;78(7):463-73.

3. Li X, et al. Psychopharmacology (Berl). 2016 May;233(10):1801-14.

4. Augier E, et al. Neuropsychopharmacology. 2016 Nov;41(12):2932-2940.

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