A-381393 是选择性、可透过血脑屏障的多巴胺D4受体拮抗剂，对人多巴胺 D4.4，D4.2和 D4.7受体的Ki分别为 1.5，1.9 和 1.6 nM，选择性是对 D1，D2，D3，D5多巴胺受体的 2700 多倍，对 5-HT2A的选择性适中，Ki=370 nM。

A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).

A-381393 potently bound to the membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3, and D5 dopamine receptors. A-381393 potently inhibited the functional activity of agonist-induced GTP-gamma-S binding assay and 1 microM dopamine-induced-Ca2+ flux in human dopamine D4.4 receptor-expressing cells, but not in human dopamine D2L or D3 receptor cells [1]. A-381393 blocked both c-Fos expression and ERK1/2 phosphorylation produced by PD168077. Treatment with A-381393 alone significantly reduced the amount of Fos immunoreactivity as compared to basal expression observed in vehicle-treated controls [2].

726174-00-1

C20H24N4

320.44

DMSO:50 mg/mL (156.04 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years