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. 2014 May 23;57(12):5318–5332. doi: 10.1021/jm5003843

Table 1. Functional and Radioligand Binding Data Obtained for NT, 1, 5a, 5b, and 6 at the NTS1 and NTS2 Receptors.

  FLIPR assay
bindinga
  NTS1
NTS2
NTS2
compd EC50b Emaxc Ke EC50 Emaxd IC50 Ki
NT 0.04 ± 0.012 100 ± 3   NAe   18.5 ± 1.2 18.9 ± 3
1 0.01 ± 0.002 114 ± 7   NA   5.4 ± 0.6 33 ± 11
5a     4.7 ± 0.8 120 ± 20 100 ± 3   62 ± 35
5b     1.5 ± 0.6 20 ± 5 100 ± 5   6 ± 2
6 NA   NA 28 ± 4 16 ± 3   33 ± 5
a

[125I]NT,

b

EC50, Ke, IC50, and Ki values are nM ± SEM.

c

Emax value is % NT.

d

Emax value is % 5b.

e

Not active.