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关于此项目
经验公式(希尔记法):
C24H24F3N5O3
化学文摘社编号:
分子量:
487.47
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable