Guanosine 5´-O-(3-Thiotriphosphate) and Cations Regulate Melatonin Receptors, and Melatonin Inhibits Cyclic AMP Production in the Spinal Cord

Autor: Liao Mx, Pang Sf, Q. Wan, Gregory M. Brown, Pang Cs
Rok vydání: 1997
Předmět:
Zdroj: Neurosignals. 6:67-76
ISSN: 1424-8638
1424-862X
DOI: 10.1159/000109111
Popis: Effects of guanosine 5'-O-(3-thiotriphosphate) (GTP gamma S) and cations on 2-[125I]iodomelatonin binding were investigated in membrane preparations of the chicken spinal cord. At concentrations of 10 and 50 mumol/l, GTP gamma S dose-dependently increased (p0.05) the equilibrium dissociation constant (Kd) and depressed (p0.05) the maximum number of binding sites (Bmax). Na+ at a concentration of 125 mmol/l significantly increased (p0.05) the Kd and decreased (p0.05) the Bmax, and Mg2+ (2.5 mmol/l) significantly increased (p0.05) the Bmax without changes in Kd. In addition, Na+ and Mg2+ affected the interactions of GTP gamma S with melatonin receptors. In the spinal cord explants, melatonin (10 nmol/l) attenuated forskolin-stimulated cyclic AMP production by 53.1%, and preincubation with pertussis toxin abolished this effect of melatonin. These results suggest that the melatonin receptors in the chicken spinal cord are linked to its second messenger via a pertussis-toxin-sensitive guanine-nucleotide-binding protein, and that cations modulate these receptors. Our studies further support a previous hypothesis that melatonin exerts a direct action on spinal cord functions.
Databáze: OpenAIRE