Loza-Huerta, Arlet published the artcileThallium-sensitive fluorescent assay reveals loperamide as a new inhibitor of the potassium channel Kv10.1, HPLC of Formula: 72509-76-3, the main research area is thallium loperamide potassium channel inhibitor; Electrophysiology; Kv10.1 potassium channel; Oncogenic channel; Thallium-sensitive fluorescent assay.
Ion channels have been proposed as therapeutic targets for different types of malignancies. One of the most studied ion channels in cancer is the voltage-gated potassium channel ether-a-́go-go 1 or Kv10.1. Various studies have shown that Kv10.1 expression induces the proliferation of several cancer cell lines and in vivo tumor models, while blocking or silencing inhibits proliferation. Kv10.1 is a promising target for drug discovery modulators that could be used in cancer treatment. This work aimed to screen for new Kv10.1 channel modulators using a thallium influx-based assay. Pharmacol. effects of small mols. on Kv10.1 channel activity were studied using a thallium-based fluorescent assay and patch-clamp electrophysiol. recordings, both performed in HEK293 stably expressing the human Kv10.1 potassium channel. In thallium-sensitive fluorescent assays, we found that the small mols. loperamide and amitriptyline exert a potent inhibition on the activity of the oncogenic potassium channel Kv10.1. These results were confirmed by electrophysiol. recordings, which showed that loperamide and amitriptyline decreased the amplitude of Kv10.1 currents in a dose-dependent manner. Both drugs could be promising tools for further studies. Thallium-sensitive fluorescent assay represents a reliable methodol. tool for the primary screening of different mols. with potential activity on Kv10.1 channels or other K+ channels.
Pharmacological Reports published new progress about Antitumor agents. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, HPLC of Formula: 72509-76-3.