pb 28

PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the ability to modulate protein-protein interaction between SARS-CoV-2 and human cells. Additionally, PB28 triggers caspase-independent apoptosis and possesses significant antitumor activity.

PB28 dihydrochloride 是一种具有选择性和高效性的 sigma 2 (σ2) 受体激动剂和 σ1 受体拮抗剂，具有抗 SARS-CoV-2 活性和抗肿瘤活性，通过调节肾癌中的 PI3K-AKT-mTOR 信号通路来抑制细胞增殖和侵袭，抑制 SK-N-SH 神经母细胞瘤细胞内质网中的钙释放，可诱导非 caspase 依赖性的细胞凋亡。