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COMPARISON OF THE EFFECTS OF ETHYLENEDIAMINE ANALOGUES AND γ‐AMINOBUTYRIC ACID ON CORTICAL AND PALLIDAL NEURONES
Author(s) -
PERKINS M.N.,
STONE T.W.
Publication year - 1982
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1982.tb08761.x
Subject(s) - bicuculline , ethylenediamine , chemistry , piperazine , depressant , stereochemistry , gaba receptor antagonist , amine gas treating , alkaloid , aminobutyric acid , pharmacology , receptor , biophysics , neuroscience , gabaa receptor , biochemistry , biology , organic chemistry
1 The actions of ethylenediamine (EDA) and structurally related compounds were investigated by microiontophoresis in Wistar rats. 2 EDA inhibited, via a bicuculline‐sensitive mechanism, the spontaneous firing rate of all cortical and pallidal cells tested. 3 The results with the analogues suggest that two amine groups are required for this neuronal depressant action whereas a carboxyl grouping is not. N‐substitution reduces the depressant effect. The length of the molecule is also critical, more than 3 methylene components seriously reducing its effectiveness. A rigid analogue of EDA, piperazine, was also active. In addition the apparent transport numbers of EDA and γ‐aminobutyric acid (GABA) were calculated, showing a close similarity between the two. 4 The results are discussed with respect to the possibility that EDA may represent a new class of GABA‐mimetics, or may indicate the existence of a novel diamine receptor mediating bicuculline‐sensitive inhibition in the rat CNS.