Figure 9

Figure 9. Expected kinetic profiles of iGluR1 Flip and Flop receptors.
(A) Expected kinetic profile of 0.5 mM glutamate (agonist) in the 1st addition followed by 20 µM LY (allosteric modulator) in the 2nd addition. (B) Expected kinetic profile of an agonist or an allosteric modulator where 20 µM LY (control potentiator) and 0.5 mM glutamate are added in 1st addition. (C) Expected kinetic profile of an antagonist where 10 µM NBQX (control inhibitor) and 0.5 mM are added in the 1st addition, followed by 20 µM LY in the second addition. In B and C, the test compounds will be added at the 1st addition with 0.5 mM glutamate, followed by 20 µM LY in the 2nd addition.

From: FLIPRâ„¢ Assays for GPCR and Ion Channel Targets

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Assay Guidance Manual [Internet].
Sittampalam GS, Gal-Edd N, Arkin M, et al., editors.
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