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BIA 10-2474

Names

[ CAS No. ]:
1233855-46-3

[ Name ]:
BIA 10-2474

[Synonym ]:
BIA-10-2474
N-Cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
5AP1ZW859M
1H-Imidazole-1-carboxamide, N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-
BIA 10-2474

Biological Activity

[Description]:

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> FAAH
Signaling Pathways >> Neuronal Signaling >> FAAH
Research Areas >> Neurological Disease

[Target]

IC50: 50-70mg/kg (FAAH, rat brain regions)[1]


[In Vitro]

ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/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 Vivo]

In January 2016, severe adverse events (SAE) occurs in the Phase I clinical 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].

[Animal admin]

Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].

[References]

[1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20.

[2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial? Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6


[Related Small Molecules]

PF-04457845 | URB597 | biochanin A | JZL195 | PF-3845 | LY2183240 | JNJ-42165279 | FAAH-IN-2 | Macamide B | FAAH inhibitor 1 | 11C-MK-3168 | FAAH-IN-1 | SA72

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
568.3±52.0 °C at 760 mmHg

[ Molecular Formula ]:
C16H20N4O2

[ Molecular Weight ]:
300.356

[ Flash Point ]:
297.5±30.7 °C

[ Exact Mass ]:
300.158630

[ LogP ]:
-0.41

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.642

[ Storage condition ]:
2-8℃

Related Compounds