Stimulation of noradrenaline release in the cerebral cortex via presynaptic N-methyl-D-aspartate (NMDA) receptors and their pharmacological characterization.
In rat brain cortex synaptosomes superfused with Mg(2+)-free solution containing glycine, [3H]noradrenaline (3H-NA) release evoked by NMDA was abolished by omission of glycine or Ca2+ and inhibited by Mg2+, the competitive and noncompetitive NMDA receptor antagonists CGP 37849 and dizocilpine (MK-801), respectively, as well as by ethanol, but was not affected by tetrodotoxin. The 3H-NA release evoked by L-glutamate was also competitively inhibited by CGP 37849. In conclusion, presynaptic NMDA receptors mediate stimulation of NA release. Ethanol probably acts at this receptor system.
Department of Pharmacology and Toxicology, University of Bonn, Federal Republic of Germany.
M
M
Göthert
K
K
Fink
D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D002118:Calcium / Q000494:pharmacology; D002540:Cerebral Cortex / Q000378:metabolism*; D016291:Dizocilpine Maleate / Q000494:pharmacology; D005971:Glutamates / Q000494:pharmacology; D018698:Glutamic Acid; D005998:Glycine / Q000494:pharmacology; D007700:Kinetics; D008274:Magnesium / Q000494:pharmacology; D008297:Male; D016202:N-Methylaspartate / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000502:physiology*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
D005971:Glutamates; D016194:Receptors, N-Methyl-D-Aspartate; C064539:2-amino-4-methyl-5-phosphono-3-pentenoic acid; D018698:Glutamic Acid; D016202:N-Methylaspartate; D016291:Dizocilpine Maleate; D015763:2-Amino-5-phosphonovalerate; D008274:Magnesium; D002118:Calcium; D005998:Glycine; D009638:Norepinephrine