Differential sensitivity to cations of the melatonin receptors in the rat area postrema and suprachiasmatic nuclei.
We studied the effects of cations on the binding of the melatonin (MT) agonist, 125I-MT, to MT receptors in the rat area postrema (AP) and suprachiasmatic nuclei (SCN), by using quantitative autoradiography in vitro. Ca2+ promoted agonist binding in the SCN but was without effect in the AP. Na+ induced a dose-dependent loss of agonist binding in both areas. This effect was more drastic in the SCN and also in the absence of divalent cations. The presence of 0.1-4.0 mM Ca2+ or Mg2+ partially and nonselectively reversed this Na(+)-elicited inhibition. The data agree with known cationic effects on agonist binding to other G protein-coupled receptors and deepen our understanding of the mammalian MT receptor.
Laitinen
J T
JT
Section on Pharmacology, National Institute of Mental Health, Bethesda, Maryland 20892.
Saavedra
J M
JM
D000818:Animals; D001345:Autoradiography; D002118:Calcium / Q000494:pharmacology*; D002413:Cations, Divalent; D002552:Cerebral Ventricles / Q000378:metabolism*; D002794:Choline / Q000494:pharmacology; D007457:Iodine Radioisotopes; D007700:Kinetics; D008274:Magnesium / Q000494:pharmacology*; D008297:Male; D008550:Melatonin / Q000378:metabolism*; D009994:Osmolar Concentration; D051381:Rats; D011919:Rats, Inbred Strains; D044094:Receptors, Melatonin; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*; D012965:Sodium Chloride / Q000494:pharmacology; D013493:Suprachiasmatic Nucleus / Q000378:metabolism*
D002413:Cations, Divalent; D007457:Iodine Radioisotopes; D044094:Receptors, Melatonin; D017981:Receptors, Neurotransmitter; D012965:Sodium Chloride; D008274:Magnesium; D008550:Melatonin; D002794:Choline; D002118:Calcium