Super-Resolution Imaging and Single Particle Tracking of Serotonin 5HT3A Receptor in Biomimetic Membranes

Abstract

then tested the GLIC-ELIC chimera with crotonic acid and picrotoxin. Crotonic acid inhibits GLIC with an IC50 of 110mM; our data indicate it binds to the extracellular domain. Picrotoxin (IC50¼2.6mM) blocks the GLIC pore(4); it likely cannot access the ELIC pore(5), but may bind to the extracellular domain (IC50¼96mM;6). These compounds were less potent than expected in the chimera (IC50>300mM). Overall the data suggest that domain specific effects may not be accurately reproduced in complex chimeras with intercommunicating domains, such as an orthosteric binding site and a pore in ligand-gated ion channels.