Many ways to dilate the P2X7 receptor pore.

ABSTRACT: The P2X7 receptor is associated with two different membrane permeabilities: a small cation conductance which opens within milliseconds, followed by the appearance of a second channel carrying higher molecular weight compounds (including organic dyes) after prolonged agonist stimulation. This activation profile has also been found in cells expressing P2X2 and P2X4 receptors; however, the P2X7 receptor-dependent pathway has the unique ability to activate pro-inflammatory signalling in macrophages. In this issue of the BJP, Marques-da-Silva et al. demonstrate that colchicine is a potent inhibitor of both P2X7 and P2X2 receptor-dependent dye uptake, without affecting the ion channels. Colchicine also blocked the pro-inflammatory signalling downstream of P2X7 receptor activation, both in vitro

SUBMITTER: Pelegrin P 

PROVIDER: S-EPMC3130938 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature