EPPTB 是TAAR1的选择性拮抗剂(对于小鼠 TAAR1 的Ki= 0.9 nM),对其他 TAARs 没有显著影响。其中TAAR1 是一种 G 蛋白偶联受体 (GPCR),能够被内源性氨基酸代谢产物非选择性的激活。
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描述
EPPTB is a selective TAAR1 antagonist.
体内活性
EPPTB prevents the reduction of the firing frequency of DA neurons induced by p-tyramine (p-tyr), a nonselective TAAR1 agonist. the EPPTB effects were absent in Taar1 knockout mice, ruling out off-target effects[2].
Cas No.
1110781-88-8
分子式
C20H21F3N2O2
分子量
378.39
别名
Epptb;Ro 5212773
储存和溶解度
DMSO:55 mg/ml (145.35 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years