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Table 3 Competition of various ligands for specific 125I-Mel binding in NIH3T3 cells transfected with either rat MT1 or MT2 cDNA

From: Gene structures, biochemical characterization and distribution of rat melatonin receptors

Compound

K i

Ratio (MT2/MT1)

MT1

MT2

I-Mel

6.22 ± 0.57 pM

4.81 ± 0.42 pM

0.77

Melatonin

290 ± 31 pM

378 ± 23 pM

1.31

6-Hydroxymelatonin

118 ± 68 nM

31.7 ± 4.9 nM

0.27

Luzindole

1.15 ± 0.19 μM

433 ± 138 nM

0.38

NAS

1.65 ± 0.42 μM

4.98 ± 2.84 μM

3.00

  1. The K i values are mean ± SEM of four experiments for each compound
  2. I-Mel 2-iodomelatonin, NASN-acetyl-5-hydroxytryptamine