Inhibition of N-methyl-D-aspartate-induced noradrenaline release by alcohols is related to their hydrophobicity.
In rat brain cortex slices, ethanol was three times more potent in inhibiting [3H]noradrenaline ([3H]NA) release evoked by N-methyl-D-aspartate (NMDA) than in inhibiting the release evoked by kainic acid. Methanol, 1-propanol, 1-butanol, 1-pentanol and 1-hexanol shared the inhibitory property of ethanol on NMDA-evoked [3H]NA release. The inhibitory potency of the alcohols, as expressed by their IC50 values, was correlated with their membrane/buffer partition coefficient. It is concluded that the inhibitory effect of the alcohols may be due to a hydrophobic interaction with the NMDA receptor system.
Fink
K
K
Institute of Pharmacology and Toxicology, University of Bonn, F.R.G.
Göthert
M
M
D000438:Alcohols / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002525:Cerebellar Cortex / Q000187:drug effects / Q000378:metabolism*; D000431:Ethanol / Q000494:pharmacology; D007608:Kainic Acid / Q000494:pharmacology; D008297:Male; D016202:N-Methylaspartate / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000494:pharmacology; D009638:Norepinephrine / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D000438:Alcohols; D000431:Ethanol; D016202:N-Methylaspartate; D007608:Kainic Acid; D009638:Norepinephrine