Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 2 de 2
Filter
Add more filters










Database
Language
Publication year range
1.
Sci Rep ; 7: 44843, 2017 03 21.
Article in English | MEDLINE | ID: mdl-28322303

ABSTRACT

Ligand gated ion channels are involved in many pathophysiological processes and represent a relevant, although challenging, target for drug discovery. We propose an innovative electro-optical approach to their analysis able to derive membrane conductance values from the local membrane potential changes imposed by test current pulses and measured by fast voltage-sensitive fluorescent dyes. We exploited the potential of this proprietary method by developing a drug testing system called "ionChannel Optical High-content Microscope" (ionChannelΩ). This automated platform was validated by testing the responses of reference drugs on cells expressing different ligand-gated ion channels. Furthermore, a double-blind comparison with FLIPR and automated patch-clamp was performed on molecules designed to act as antagonists of the P2RX7 receptor. ionChannelΩ proved highly reliable in all tests, resulting faster and more cost-effective than electrophysiological techniques. Overall, ionChannelΩ is amenable to the study of ligand gated ion channels that are receiving less attention due to limitations in current assays.


Subject(s)
Drug Discovery/methods , Ion Channel Gating/drug effects , Ligand-Gated Ion Channels/metabolism , Microscopy/methods , Optical Imaging/methods , Automation, Laboratory , Cell Membrane Permeability/drug effects , High-Throughput Screening Assays , Humans , Ligands , Membrane Potentials/drug effects , Microscopy, Fluorescence/methods , Reproducibility of Results
SELECTION OF CITATIONS
SEARCH DETAIL
...