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The σ 1 receptor is an important target for CNS disorders. We previously identified a σ 1 ligand TZ3108 having highly potent ( K  i-σ1 = 0.48 nM) and selective affinity for σ 1 versus σ 2 receptors. TZ3108 was 18 F-labeled with F-18 for in vivo evaluation. Biodistribution and blocking studies of [ 18 F]TZ3108 in male Sprague-Dawley rats demonstrated high brain uptake, which was σ 1 -specific with no in vivo defluorination. MicroPET studies in cynomolgus macaques showed high brain penetration of [ 18 F]TZ3108; the regional brain distribution was consistent with that of the σ 1 receptor. Pseudo-equilibrium in the brain was reached ~ 45 min post-injection. Metabolite analysis of [ 18 F]TZ3108 in NHP blood and rodent blood and brain revealed that ~ 70% parent remained in the plasma of NHPs 60 min post-injection and the major radiometabolite did not cross the blood-brain barrier in rats. In summary, the potent, selective and metabolically stable σ 1 specific radioligand [ 18 F]TZ3108 represents a potentially useful PET radioligand for quantifying the σ 1 receptor in the brain.

Radiosynthesis and in vivo evaluation of a novel σ1 selective PET ligand

Radiosynthesis and in vivo evaluation of a novel σ₁ selective PET ligand