1354030-51-5

UNC9994 is a β-arrestin-biased dopamine D? receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%). UNC9994 has robust in vivo antipsychotic drug-like activities. Functionally selective G protein-coupled receptor (GPCR) ligands, which differentially modulate canonical and noncanonical signaling, are extremely useful for elucidating key signal transduction pathways essential for both the therapeutic actions and side effects of drugs.

UNC9994 是 Aripiprazole 的类似物，是一种功能选择性 β-阻遏蛋白偏向的多巴胺 D2 受体(β-arrestin-biased dopamine D2 receptor) 激动剂，对于 β-阻遏蛋白-2 向 D2 受体的募集的 EC50 <10 nM。UNC9994 同时是 β-arrestin-2 易位的部分激动剂和 Gi 调节的 cAMP 产生的拮抗剂。具有抗精神病活性。