TABLE 5

Pharmacological profile of partial agonists/antagonists on hMT1, hMT2, and native melatonin receptors

All values are from Dubocovich et al. (1997) except as noted otherwise.

Melatonin Receptor Ligands2-[125]IMLT Binding[3H]DA Release in Rabbit Retina MT2 (pA2)GTPγS Binding
Ratio hMT1/ hMT2hMT1 pKihMT2 pKihMT1KBhMT2KBRatio hMT1/ hMT2
4P-CADOT3626.59.19.3
4P-ADOT3306.28.98.8
4P-PDOT3116.38.89.5
K185a1327.29.3N.D.
5-Methoxyluzindole1307.59.610.2
S 24014b1257.59.67.38.830
GR 1281071137.09.110.2
N 0891916.18.07.7
DH97c896.18.0N.D.
N 0890566.27.97.5
N 0889316.88.37.8
Luzindole166.88.07.7
N-Acetyltryptamine156.77.98.0
GR 135533156.57.78.6
S 20928b3.17.958.227.17.97.1
S 22153b1.98.858.158.57.92.5
5-HEATd0.27.87.1N.D.
S 25567b0.168.57.78.47.70.23
S 26284b0.018.85787.40.28
S 26131b0.018.856.98.36.80.04

  • IMLT, iodomelatonin; DA, dopamine; 4P-CADOT, 4-phenyl-2-chloro-acetamidotetraline; N.D., not determined; 5-HEAT, 5-hydroxyethoxy-N-acetyltryptamine.

  • ↵a Values from Faust et al., 2000.

  • ↵b Audinot et al., 2003.

  • ↵c Teh and Sugden, 1999.

  • ↵d Nonno et al., 2000.