Sipagladenant (Compound I) is an orally active inverse agonist targeting the adenosine receptor A2A [1]. It possesses potential for utilization in research pertaining to frontal lobe dysfunction [2].

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).