Skip to main content

Advertisement

Table 1 Binding properties of ligands to soluble 6 × His-ATD2B protein and their inhibition on heterologously expressed NR1-1a/NR2B receptors in Xenopus oocytes.

From: Structural insights into phenylethanolamines high-affinity binding site in NR2B from binding and molecular modeling studies

Ligand K D (nM)   IC 50 (nM)  
RO25,6981 7 ± 3 (n = 5) 59 ± 1 (n = 22)
Ifenprodil 60 ± 18 (n = 5) 105 ± 9 (n = 20)
Haloperidol 3094 ± 940 (n = 5) 2762 ± 363 (n = 18)
  1. Dose-titration binding constants of RO25,6981, ifenprodil and haloperidol performed on Buffer -9 refolded 6 × His-ATD2B protein determined from CD. Values are mean ± S.E. of the KD values from five experiments using proteins obtained from at least two independent batches of bacteria induction. Rat NR1 and NR2B subunits were coexpressed in Xenopus oocytes. NR2B-selective antagonists' inhibition of current responses induced by glutamate and glycine at pH7.3 were analyzed to obtain the mean-fitted IC50 values with n representing number of oocytes recorded.