Description
PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist.? Selective for σ2 over σ1 (approx 30-40x).1,2 PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin.3? PB28 potently inhibited Kv2.1 currents in a σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5
References
Berardi et al. (1996), New s and 5-HT1A Receptor Ligands: w-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176
Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as s Receptor Ligands with Agonist s2 Activity; J. Med. Chem. 47 2308
Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a s2 agonist and s1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Cancer Ther. 5 1807
Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
