EJNMMI Research

Table 1 Physical and pharmacological parameters of FTC146, NR2B-SMe, NR2B-Me, and their enantiomers

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	Ref	cLogD_7.4	pK_a	GluN2B K_i (nM)	σ1 K_i (nM)	σ2 inhibition^a (%)	σ2 K_i (nM)
FTC146	[27]	1.45	10.4		.0025		364
NR2B-SMe	[26]	3.41	5.03	2.2		90
(R)-NR2B-SMe	[26]				88		110
(S)-NR2B-SMe	[26]				24		140
NR2B-Me		3.27	5.04	4.9		91
(−)-NR2B-Me					42		110
(+)-NR2B-Me					130		100

^aAt 10 µmol

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