2021 - Taspine is a natural product that suppresses P2X4 receptor activity via phosphoinositide 3-kinase inhibition
Port-a-Patch Pre-Print Publication in British Journal of Pharmacology (2021)
Bin Nadzirin I., Fortuny-Gomez A., Ngum N., Richards D., Ali S., Searcey M., Fountain S.J.
British Journal of Pharmacology (2021) doi: 10.1111/bph.15663
Background & purpose
P2X4 is a ligand-gated cation channel activated by extracellular ATP, involved in neuropathic pain, inflammation and arterial tone.
Natural products were screened against human or mouse P2X4 activity using fura-2 loaded 1321N1 cells for measurement of intracellular Ca2+ responses; whole-cell currents were measured by patch clamp electrophysiological. Human primary macrophage chemokine release was used to assess effect of taspine on inflammatory cell function. An enzymatic assay was performed to assess the effect of taspine on recombinant PI3-kinase.