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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.
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