Table 1 Potency and relative agonistic activity (RAA) of typical MTNR ligands in mammals for medaka MTNRs
From: Vertebrates originally possess four functional subtypes of G protein-coupled melatonin receptor
Ligand | MTNR1a | MTNR1b | MTNR1c | MTNR1a-like | ||||
|---|---|---|---|---|---|---|---|---|
Potency (M) | RAA (%) | Potency (M) | RAA (%) | Potency (M) | RAA (%) | Potency (M) | RAA (%) | |
Melatonin | 4.8 ± 2.0 × 10−10 | 100 ± 3.8 | 1.9 ± 0.49 × 10−9 | 100 ± 4.4 | 6.2 ± 0.61 × 10−11 | 100 ± 1.8 | 2.2 ± 0.63 × 10−8 | 100 ± 2.9 |
2-Iodo melatonin | 2.7 ± 1.7 × 10−11 | 95.8 ± 6.9 | 3.9 ± 0.32 × 10−11 | 101.4 ± 2.8 | 1.3 ± 0.39 × 10−11 | 111.8 ± 3.2 | 4.0 ± 1.1 × 10−10 | 69.3 ± 6.8 |
4P-PDOT | 4.7 ± 0.63 × 10−9 | 67.4 ± 6.1 | NC | ND | NC | ND | 1.2 ± 0.24 × 10−7 | 68.7 ± 6.4 |
Luzindole | 3.3 ± 0.21 × 10−7 | 68.2 ± 3.8 | NC | ND | NC | 117.6 ± 11.5 | NC | 83.1 ± 13.4 |
