Sch412348 is a potent competitive the human adenosine A2A receptor antagonist with Ki of 0.6 nM and has >1000-fold selectivity over all other adenosine receptors.

A2A receptor:ki： 0.6 nM

Sch412348 is determined to have KB values of 0.3 nM, respectively at the A2A receptor; the value are in good agreement with the Ki values determined in radioligand binding assays. A similar functional assay with A2B receptor-expressing cells is used to demonstrate selectivity over A2B receptors.Sch412348 also completely antagonizes cAMP in cells expressing the recombinant human A2A receptor. The KB value for Sch412348 is 273 nM, indicating that Sch412348 is 910-fold selective for the A2A receptor over the A2B receptor.

Administering Sch412348 orally (0.1-1 mg/kg) to rats enhances the effects of 3,4-dihydroxy-L-phenylalanine (L-Dopa) in inducing contralateral rotations after creating lesions in the medial forebrain bundle with 6-hydroxydopamine, and significantly diminishes the cataleptic effects caused by haloperidol. Furthermore, Sch412348 (1 and 3 mg/kg) was observed to reduce haloperidol-induced catalepsy at both 1 hour [F(3,20)=3.9, p<0.05] and 4 hours [F(3,20)=7.5, p<0.01] post-administration in a dose-dependent manner. Additionally, Sch412348 (0.1-1 mg/kg) notably decreases the duration of immobility in mice during the tail suspension test (TST) at a 1 mg/kg dose [F(2,51) =10.6, p<0.01]. The substance also increased activity levels in mice [F(4,27)=2.9, p<0.05], particularly in the 0.3 and 3 mg/kg treatment groups, which showed significantly higher activity than those treated with a vehicle, with the 1 mg/kg dose nearing significance (p=0.052).