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(Rac)-Tavapadon((Rac)-PF-06649751;(Rac)-CVL-751)是有效的,选择性非儿茶酚多巴胺D1受体(dopamineD1receptor)激动剂。(Rac)-Tavapadon在GS激活试验中显示出强大的完全激动作用,在β-arrestin2募集试验中显示出部分激动作用(GS-cAMP,EC50=0.8nM;β-arrestin2,EC50=68nM)。(Rac)-Tavapadon具有抗帕金森病活性。
(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].
(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1].
[1]. Michael L Martini, et al. Designing Functionally Selective Noncatechol Dopamine D 1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci. 2019 Sep 18;10(9):4160-4182.
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