A-381393 is a potent, selective, brain penetrate dopamine D 4 receptor antagonist, with K i s of 1.5, 1.9 and 1.6 nM for human dopamine D 4.4 , D 4.2 , and D 4.7 receptor, respectively, >2700-fold selectivity over D 1 , D 2 , D 3 and D 5 dopamine receptors. A-381393 shows moderate affinity for 5-HT 2A (K i , 370 nM).
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