Rank-order of potencies of galanin-related peptides for the inhibition of forskolin-stimulated cAMP production, stimulation of GTPγS binding and inhibition 125I-human galanin binding in cells expressing human GALR1 receptors
| Peptide | 125I-Human Galanin Binding (Ki, pM) | ↓ cAMP Production (IC50, pM) | ↑ GTPγS Binding (EC50, pM) | |||
|---|---|---|---|---|---|---|
| Membranes | Whole cells | Whole cells | Membranes | |||
| M35 | 11.5 ± 0.9 (3) | 169.9 ± 63.7 (4) | 66.7 ± 8.2 (3) | 290 ± 80 (4) | ||
| Porcine galanin | 25.2 ± 5.7 (3) | 226.8 ± 37.9 (4) | 53.3 ± 13.2 (10) | 660 ± 140 (3) | ||
| Human galanin | 30.9 ± 3.8 (3) | 232.0 ± 33.9 (4) | 31.3 ± 9.4 (3) | 630 ± 95 (9) | ||
| M15 | 27.4 ± 3.6 (3) | 255.5 ± 64.5 (2) | 105 ± 35 (2) | 490 ± 180 (4) | ||
| C7 | 81.8 ± 16 (6) | 685.0 ± 157.2 (4) | 386.7 ± 89.7 (3) | 6100 ± 1250 (2) | ||
| Galanin 1–16 | 105.9 ± 8.0 (3) | NT | 443.3 ± 104.9 (3) | 2730 ± 730 (5) | ||
| M40 | 109.4 ± 13.0 (3) | 713.0 ± 68.9 (4) | 272.8 ± 25.7 (4) | 1590 ± 460 (4) | ||
| Human NPY | NA | NT | NA | NT | ||
Values represent the mean ± S.E.M. for the number (n) of experiments indicated. NA, not active; NT, not tested.