BIA10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂，与人类内源性大麻素系统相互作用，可增加中枢神经系统和外周组织，对大鼠大脑不同区域的IC50值为50至70mg/kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。

BIA10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474 interacts with the human endocannabinoid system. BIA 10-2474 was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70 mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[1].

In January 2016, severe adverse events (SAE) occurs in the Phase I Clinicalal trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2].

1233855-46-3

C16H20N4O2

300.362

BIA10-2474

DMSO:4 mg/mL(13.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years