Sipagladenant

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist[1]. Sipagladenant can be used in frontal lobe dysfunction research[2].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Sipagladenant (oral administration; 0.3 mg/kg; once) treatment improves cognitive impairment due to a decline in dopamine function in the medial prefrontal cortex[2]. Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve alternation behavior[2]. Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve gait parameters[2]. Animal Model: Medial prefrontal dopaminerjic terminal-lesioned CD(SD) IGS male rat[2] Dosage: 0.3 mg/kg Administration: Oral administration; 0.3 mg/kg; once Result: Showed longer exploration time of the novel object (65.03%) than that of the familiar object (34.97%) (p<0.001). Animal Model: ICR mice with cognitive impairment and/or movement disoder[2] Dosage: 0.1 mg/kg Administration: Oral administration; 0.1 mg/kg; once Result: Showed a significantly high alternation behavior (69.5%) as compared to the vehicle administration group (59.6%) (p<0.01). Animal Model: ICR mice with cognitive impairment and/or movement disoder[2] Dosage: 0.1 mg/kg Administration: Oral administration; 0.1 mg/kg; once Result: Showed a significantly large maximum contact area and gait area of the left hindpaw as compared to the vehicle administration group (p<0.05), tendency of the maximum contact area and gait area of the right forepaw being large (p<0.1).

[1]. https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl127.pdf?sfvrsn=8544ca1e_3&download=true

[2]. Horita, Takako. THERAPEUTIC AGENT FOR FRONTAL LOBE DYSFUNCTION, WO2016148308A1.