中文名称:

N/A

中文同义词:

英文名称:

AC-5216

英文同义词:

EMapunil;XBD-173;N-Benzyl-N-ethyl-2-(7-Methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetaMide;9H-Purine-9-acetaMide,N-ethyl-7,8-dihydro-7-Methyl-8-oxo-2-phenyl-N-(phenylMethyl)-;AC 5216 (Emapunil);N-Ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-9H-purine-9-acetamide;Emapunil(AC-5216);AC-5216

CAS号:

226954-04-7

分子式:

C23H23N5O2

分子量:

401.46

EINECS号:

相关类别:

小分子抑制剂;小分子抑制剂，天然产物;活性分子;Inhibitors

Mol文件:

226954-04-7.mol

储存条件 

2-8°C

形态

powder

颜色

white to beige

生物活性

Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173)是一种新型的 mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) 配体。Emapunil(AC-5216) 对大鼠全脑制备的 MBRs 具有高亲和力，Ki值为0.297 nM，在大鼠神经胶质瘤细胞和人神经胶质瘤细胞上的IC50值分别为 3.04 nM和 2.73 nM。

靶点

Target Value mMBR(Brain) (Cell-free assay) 0.297 nM(Ki) MBR (human glioma cells-based assay) 2.73 nM MBR (rat glioma cells-based assay) 3.04 nM

Target

Value

mMBR(Brain) (Cell-free assay)

0.297 nM(Ki)

MBR (human glioma cells-based assay)

2.73 nM

MBR (rat glioma cells-based assay)

3.04 nM

体内研究

Emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, p.o.) produces anti-anxiety effects in the Vogel-type conflict test in rats, and in the light/dark box and social interaction tests in mice. Emapunil (AC-5216, 3-30 mg/kg, p.o.) reduces the immobility time, and this effect was blocked by PK11195. Emapunil (AC-5216, 1-100 mg/kg, p.o.) produces no distinct change in the rat electroencephalogram. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) causes significant suppression of the enhanced anxiety and contextual fear induced in post-TDS rats. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) alleviates the enhanced anxiety and fear response in a time-dependent sensitization (TDS) procedure, a rat PTSD animal model. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) reverses the increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats. Animal Model: Rats. Dosage: 0.1-3 mg/kg. Administration: P.O.. Result: Significantly increased the number of shocks that rats received. Significantly increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, p.o. (P<0.1).

Animal Model:

Rats.

Dosage:

0.1-3 mg/kg.

Administration:

P.O..

Result:

Significantly increased the number of shocks that rats received. Significantly increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, p.o. (P<0.1).