TABLE 3

In vitro pharmacological profile of NOP selective antagonists

human NOProdent NOP
receptor bindingNOP/G-protein[35S]GTPγSCa2+ mobilizationmVDrVD
pKiselectivitypKB/pA2pKB/pA2pKB/pA2pKB/pA2pKB/pA2
[Nphe1]8.39a269partial agonistb7.33c6.29d6.04a6.16a
UFP-10110.24e> 10007.66b8.85c7.66d7.29e7.30e
J-1133979.15f1477.95b9.08f7.32d7.81g7.77g
SB-6121119.18h> 10008.96b9.70h8.16d8.50h8.20h
C-249.62i7949.11b9.98i8.73i8.44i8.28i
  • a (Calo’ et al., 2000b), b (Malfacini et al., 2015), c (McDonald et al., 2003b), d (Camarda et al., 2009), e (Calo’ et al., 2002b), f (Trapella et al., 2006), g (Bigoni et al., 2000), h (Spagnolo et al., 2007), i (Fischetti et al., 2009b). Underscored data indicate pA2 values obtained from Schild plots.