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Table 2 Binding affinities at NPY Y1- and Y2-receptors and Y1-related functional characteristics

From: Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers

Analog number Binding affinitya Functional assay
  Y 1 Y 2 cAMP for Y 1
DOTA-free analogs
1 11 ± 7 > 1,000 Antagonist
3 9.0 ± 3 > 1,000 Antagonist
5 143 ± 20 > 1,000 ND
7 19 ± 5 > 1,000 Antagonist
9 127 ± 50 > 1,000 Antagonist
DOTA-coupled analogs
2 143 ± 37 > 1,000 Antagonist
4 294 ± 33 > 1,000 Antagonist
6 > 1000 > 1,000 ND
8 29 ± 7 > 1,000 Antagonist
10 283 ± 52 > 1,000 Antagonist
11 13 ± 3 > 1,000 Antagonist
  1. Functional characteristics for free and DOTA-coupled dimeric peptide NPY analogs. aIC50 values in nanomolars; mean ± SEM; n ≥ 3. ND, not determined.