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  • Title: GABAB-receptor-mediated actions of baclofen in rat isolated neocortical slice preparations: antagonism by phosphono-analogues of GABA.
    Author: Kerr DI, Ong J, Johnston GA, Prager RH.
    Journal: Brain Res; 1989 Feb 20; 480(1-2):312-6. PubMed ID: 2540879.
    Abstract:
    Baclofen, 3-amino-propylphosphonic acid (3-APPA), and beta-phenyl-GABA (BPG), each reduced the frequency of spontaneous paroxysmal discharges in rat neocortical slices maintained in Mg2+-free medium, reversibly antagonised by phaclofen and 4-amino-butylphosphonic acid (4-ABPA). At lower concentrations, not influencing the discharges, both 3-APPA and BPG also reversibly antagonised this action of baclofen. However, des-chloro-phaclofen was inactive. Thus, phaclofen and 4-ABPA are GABAB-receptor antagonists in neocortex, whereas both 3-APPA and BPG have partial agonist/antagonist activity at cortical GABAB-receptors.
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