Inhibition of N-methyl-D-aspartate-induced noradrenaline release by alcohols is related to their hydrophobicity

• Published in: European journal of pharmacology Vol. 191; no. 2; p. 225
• Main Authors: Fink, K, Göthert, M
• Format: Journal Article
• Language: English
• Published: Netherlands 27-11-1990
• Subjects: Alcohols - chemistry; Alcohols - pharmacology; Animals; Cerebellar Cortex - drug effects; Cerebellar Cortex - metabolism; Ethanol - pharmacology; Kainic Acid - pharmacology; Male; N-Methylaspartate - antagonists & inhibitors; N-Methylaspartate - chemistry; N-Methylaspartate - pharmacology; Norepinephrine - metabolism; Rats; Rats, Inbred Strains
• ISSN: 0014-2999
• DOI: 10.1016/0014-2999(90)94152-N

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.