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Table 2 In vitro characteristics of SIG343 and SIG353

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

Parameters

Compound

SIG343

SIG353

Affinity (nM)

  

σ1 a

1,600

266

σ2 a

8

2.4

Opioid, non-selectiveb

>104

>104

Dopamine, non-selectiveb

>104

>104

Serotonin, non-selectiveb

>104

>104

CB1, non-selectiveb

>104

>104

Muscarinic, non-selectiveb

>104

>104

Selectivity

  

σ21

200

110

Lipophilicity

  

LogPb

3.11 ± 0.08

3.47 ± 0.09

  1. a K i, determined by ANSTO LifeSciences; b IC 50, determined by Caliper LifeSciences.