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Table 2 In vitro and in vivo pharmacological parameters of GluN2B ligands

From: Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors

Ligand

Ki for GluN2B (nM)

ED50 in rat whole brain in vivo

11C-(S)-NR2B-SMea

11C-(−)-NR2B-Me

11C-(+)-NR2B-Me

18F-FTC146

(nmol/kg)

NR2B-SMe

2.0

9.5

  

1064

Ro-25-6981

9.0

29

34

45

 

CO101,244

43

74

 

41

 
  1. aRef. [26]
  2. bRef. [36]
  3. cRef. [37]