Name: Dopamine D3 receptor antagonist-3
Brand: TargetMol
SKU: T212099
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

10-14周

50 mg

待询

10-14周

生物活性

产品描述	Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist (PAM-antagonist) of the D3 dopamine receptor (D3R) that can cross the blood-brain barrier. It demonstrates antagonistic activity in D3R-mediated β-arrestin recruitment assays with an IC50 of 2.5 μM and Kb of 0.49 μM, and in D3R-mediated Go-BRET assays with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 is applicable for the study of neuropsychiatric disorders, including substance use disorders.
靶点活性	Dopamine D3 receptor:0.49 μM (Kd)
体外活性	Dopamine D3 receptor antagonist-3 (Compound 6a) 在人、小鼠和大鼠中表现出良好的微粒体稳定性，对 hERG 通道显示 IC50 值大于 10 μM，表明无活性。
体内活性	化合物6a (40 mg/kg，腹腔注射，单次给药) 作为Dopamine D3 receptor antagonist-3，在脑部具有良好的渗透性，脑半衰期达到3.65小时，C maxs为3183 ng/g (6.5 μM)。