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. 2019 Oct;71(4):571–595. doi: 10.1124/pr.119.017863

TABLE 3.

Recent data on allosteric effect of Na+

Receptor Allosteric Effect [Na+] Estimate of Na+ Affinity PDB ID (Na+ in Structure) Reference
DRD4 Agonist NAM, reduce basal activity KB = 98 mM 5WIV (Na+) Wang et al. (2017)
DRD2 Agonist NAM, control of other allosteric ligands KB = 123.1 mM 6CM4 Wang et al. (2017), Draper-Joyce et al. (2018)
DRD3 Agonist NAM KB = 76 mM 3PBL Wang et al. (2017)
MOR Agonist NAM, control of other allosteric ligands KB = 7.3 mM 4DKL Wang et al. (2017), Livingston et al. (2018)
DOR Agonist NAM, control of other allosteric ligands KB = 24.3 mM 4N6H (Na+) Wang et al. (2017)
A2AR Agonist NAM KB = 32.4 mM 4EIY (Na+) Wang et al. (2017)
CLTR1 Receptor thermostability EC50 = 39 mM 6RZ4, 6RZ5 (Na+) Luginina et al. (2019)
BLT1 Agonist NAM EC50 < 200 mMa 5X33 (Na+ site blocked by ligand) Hori et al. (2018)
V1b Agonist NAM, required for IP3 signaling EC50 < 50 mMa n/a Koshimizu et al. (2016)
OXTR Agonist NAM EC50 < 200 mMa n/a Schiffmann and Gimpl (2018)
H1R Agonist NAM EC50 < 100 mMa 3RZE Hishinuma et al. (2017)
NTSR1 Agonist NAM EC50 = 43 mM 4BUO White et al. (2018)
ETA Agonist NAM EC50 = 245 mM n/a Shihoya et al. (2017)
a

Approximately estimated from Na+ titration curves in the referenced papers.