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

EJNMMI Research

Table 3 In vitro and in vivo pharmacological parameters for σ1 receptor ligands (not identified as agonists)

σ1 Ligand	K_i for σ1 (nM)^a	K_i for σ2 (nM)^b	ED₅₀ in rat whole brain in vivo
			¹⁸F-FTC146	¹¹C-(−)-NR2B-SMe	¹¹C-(+)-NR2B-Me	¹¹C-(−)-NR2B-Me
			(nmol/kg)
FTC146	0.0025^c,d	364	46	2571	725	> 1000
BD1047	0.9^e	47	169	> 1000	555	900

^aReference radioligand ³H-pentazocine, except that ¹⁸F-FTC146 was used for FTC146
^bReference radioligand ³H-DTG
^cRef. [27]
^dRef. [38]
^eRef. [39]