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Figure 3 | BMC Pharmacology

Figure 3

From: Extrinsic factors regulate partial agonist efficacy of strychnine-sensitive glycine receptors

Figure 3

Glycine receptors expressed in different expression systems have similar 'functional' strychnine binding. Cells were pre-treated for 30 seconds with strychnine alone then exposed to a strychnine admixture with an EC50 concentration of glycine. (A) Strychnine-mediated inhibition of glycine-gated currents of GlyRα2 homomers expressed in HEK 293 (□; IC50 = 78.2 ± 13.5 nM) and L-cells (■; 33.1 ± 6.3 nM). (B) Strychnine-mediated inhibition of glycine-gated currents of GlyRα2β heteromers expressed in HEK 293 (; 37.9 ± 7.9 nM) and L-cells (; 23.2 ± 4.6 nM). (C) Functional KB values were calculated from IC50 values for individual cells using the Cheng-Prusoff relationship and glycine affinity/Hillslope data represented in Figure 1. Average KB values are shown for each subunit combination in the two expression systems. There was no significant effect of subunit compositions or expression system.

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