Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.

ABSTRACT:

Background and purpose

In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of ivermectin is a species-specific phenomenon.

Experimental approach

Complementary electrophysiological and fluorometric methods were applied to evaluate the effect of ivermectin on recombinantly expressed and on native P2X7 receptors. A biophysical characterization of ionic currents and of the pore dilation properties is provided.

Key results

Unexpectedly, ivermectin potentiated currents in human monocyte-derived macrophages that endogenously express hP2X7 rec

SUBMITTER: Norenberg W 

PROVIDER: S-EPMC3448913 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature