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UCSF924是一种有效且特异性的多巴胺D4受体(DRD4)部分激动剂,EC50值为4.2nM。UCSF924具有高亲和力,对DRD4的Ki值为3nM,而对D2,D3或F261V/L328FD4突变体没有可测的亲和力。对于Gαi/o信号传导,UCSF924是抑制蛋白的7.4倍偏倚。
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole[1].
[1]. Wang S, et al. D4 dopamine receptor high-resolution structures enable the discovery of selective agonists. Science. 2017 Oct 20;358(6361):381-386.
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