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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.