TABLE 1

sstr-2 and sstr-4 Affinities for Various Agonist 19F-Fluoroethyltriazole-Tyr3-Octreotate Ligands Expressed as Concentration at Which Half-Maximal Receptor Activation Occurs (Half-Maximal Effective Concentration, EC50)

Predicted agonist EC50 potency value
Compound identitysstr-2sstr-4
Somatostatin5.6 nM3.8 nM
19F-FET-G-PEG-TOCA19.0 nM>10 mM
19F-FETE-PEG-TOCA12.0 nM>10 mM
19F-FET-βAG-TOCA4.7 nM8.6 mM
19F-FET-G-TOCA6.9 nM5.4 mM
19F-FETE-TOCA4.1 nM6.5 mM
19F-FET-βAG-[W-c-(CTFTYC)K]220 nMND
  • ND = could not be determined because of lack of activity.