Barbadin 是一种选择性 β-arrestin/β2-adaptin 相互作用抑制剂，β-arrestin1和 β-arrestin2 的 IC50 值分别为 19.1 μM 和 15.6 μM。Barbadin 阻断激动剂促进 β2-adrenergic, V2-vasopressin 和 angiotensin-II type-1 受体的内吞作用。
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors[1].
[1]. Beautrait A, et al. A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling. Nat Commun. 2017 Apr 18;8:15054. doi: 10.1038/ncomms15054.
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