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.
Göthert
M
M
Department of Pharmacology and Toxicology, University of Bonn, Federal Republic of Germany.
Fink
K
K
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