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. Author manuscript; available in PMC: 2015 Oct 1.
Published in final edited form as: Neuropharmacology. 2014 May 27;85:57–66. doi: 10.1016/j.neuropharm.2014.05.022

Figure 2. Mutations in the modulator binding site differentially perturb receptor desensitization.

Figure 2

Outside-out membrane patches pulled from HEK293 cells transiently expressing WT GluA2o (flop) receptor isoforms and point mutations in the allosteric modulator binding site were screened for modulator efficacy, using 10 mM glutamate alone or in the presence of CTZ, CX614, CMPDA and CMPDB. Efficacious modulation of desensitization is observed as an absence of peak current decay during a prolonged (500 ms) pulse of 10 mM glutamate in the presence of 10 (CMPDA and B) or 100 (CTZ, CX614) μM. Traces shown are normalized to the largest peak amplitude, which was 500 pA, and ranged from10–500 pA. WT traces are re-published from Timm et al., 2011 with permission from the publisher.