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中文名称

CAY10651 (1 mg)

英文名字
CAY10651, 3-fluoro-5-(2-methylbenzo(d)thiazol-5-yl)-benzonitrile
供应商
Cayman
产品货号
10820-1
产品报价
¥420/1 mg
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背景资料
Glutamate, the major excitatory neurotransmitter in the CNS, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors -mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical models of disease, including pain, anxiety, gastresophageal reflux disease, Parkinson s associated dyskinesia, and fragile X syndrome, as well as in animal models of drug addiction. CAY10651 is a noncompetitive antagonist -negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay. A 10 uM concentration of CAY10651 results in a near complete blockade of the glutamate response in cortical astrocytes. A 30 mg/kg dose of CAY10651 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.
产品描述
A noncompetitive antagonist of mGlu5 -IC50 = 61 nM; Ki = 477 nM); 10 uM results in a near complete blockade of the glutamate response in cortical astrocytes; 30 mg/kg in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction
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保存建议
-20
其他
Cayman Chemical
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