Skip to main content

Advertisement

Table 1 Overall review of reported selective σ2 ligands for PET and SPECT

From: Synthesis and biological characterisation of 18F-SIG343 and 18F-SIG353, novel and high selectivity σ2 radiotracers, for tumour imaging properties

Ligands Radiolabel K i aor IC 50 b(nM) Comments References
  σ 1 σ 2   
125I 554a 1.0a Tumour-to-muscle ratio = 6 (4 h, EMT-6 tumoured mice) [41]
76Br 5484a 12a Tumour-to-muscle ratio = 2 (2 h, EMT-6 tumoured mice) [42]
76Br 12900a 8.2a Tumour-to-muscle ratio = 8 (2 h, EMT-6 tumoured mice) [42]
11C 3078a 10a Tumour-to-muscle ratio = 3 (1 h, EMT-6 tumoured mice) [43]
18F 330a 6.9a Tumour-to-muscle ratio = 3 (2 h, EMT-6 tumoured mice) [40]
18F 2150a,c 0.26a,c Tumour-to-muscle ratio = 8 (2 h, EMT-6 tumoured mice) [40]
125I, 18F 2.8a,d Tumour-to-muscle ratio = 8 (2 h, Line 66 breast tumoured mice) [44]
18F 1711a 0.8a Tumour-to-muscle ratio = 2 (2 h, EMT-6 tumoured mice) [45]
18F 6b 2b Brain-to-muscle ratio = 3 (2 h, naïve mice) [45]
  1. a K i, determined by ANSTO LifeSciences; b IC 50, determined by Caliper LifeSciences; csubtype affinity and selectivity performed in EMT-6 cell line; daffinity performed in line 66 cell line, selectivity not determined.