Antagonism of ethanol-induced depressant effects by 4-aminopyridine in the central nervous system of the rat.
Intraperitoneal injection of ethanol (2 g/kg) produced significant motor impairment in rats, as measured by performance on the tilting plane. Administration of 3 mg/kg 4-aminopyridine (4-AP) antagonized the depressant effect of ethanol on motor performance. Using slices of hippocampus, in vitro, 4-aminopyridine (10-100 microM) also antagonized the ethanol-induced depressant effect on orthodromically-elicited population spikes in the CA1 pyramidal cell layer. This antagonism appears to result from the ability of 4-aminopyridine to enhance release of transmitter in both excitatory and inhibitory neurones. Due to a number of unwanted side effects, further evaluation of 4-aminopyridine and its analogues needs to be done before it can be considered useful in the management of acute intoxication with ethanol.
D015761:4-Aminopyridine; D000200:Action Potentials / Q000187:drug effects; D000631:Aminopyridines / Q000494:pharmacology*; D000818:Animals; D003864:Depression, Chemical; D004558:Electric Stimulation; D000431:Ethanol / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D006624:Hippocampus / Q000187:drug effects* / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D009043:Motor Activity / Q000187:drug effects*; D051381:Rats; D011919:Rats, Inbred Strains
D000631:Aminopyridines; D000431:Ethanol; D015761:4-Aminopyridine