4-Aminopyridine inhibits synaptosomal plasma membrane protein phosphorylation in vitro: effect of the selective NMDA-antagonist 2-amino-5-phosphonovalerate.
Phosphorylation of synaptosomal plasma membranes from rat hippocampus in the presence of the convulsant drug 4-aminopyridine resulted in the inhibition of the phosphorylation of the nervous tissue specific protein kinase C substrate protein B-50 (48 kDa) and the alpha-subunit of calcium/calmodulin-dependent protein kinase II (50 kDa). Preincubation of SPM with 2-amino-5-phosphonovalerate prevents the inhibition of B-50 phosphorylation by 4-aminopyridine, but had no effect on the inhibition of 50 kDa phosphorylation. 2-Amino-5-phosphonovalerate is known to be a specific N-methyl-D-aspartate antagonist and has anti-epileptic activity in vitro and in vivo. Several other anti-epileptic drugs tested did not influence the 4-aminopyridine-induced inhibition of protein phosphorylation.
D015763:2-Amino-5-phosphonovalerate; D015761:4-Aminopyridine; D000631:Aminopyridines / Q000037:antagonists & inhibitors*; D000818:Animals; D006624:Hippocampus / Q000187:drug effects* / Q000378:metabolism; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects; D008297:Male; D008565:Membrane Proteins / Q000378:metabolism*; D008970:Molecular Weight; D009419:Nerve Tissue Proteins / Q000378:metabolism*; D010750:Phosphoproteins / Q000378:metabolism*; D011494:Protein Kinases / Q000378:metabolism; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000187:drug effects; D013570:Synaptic Membranes / Q000187:drug effects*; D014633:Valine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000631:Aminopyridines; D007473:Ion Channels; D008565:Membrane Proteins; D009419:Nerve Tissue Proteins; D010750:Phosphoproteins; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D015763:2-Amino-5-phosphonovalerate; D015761:4-Aminopyridine; D011494:Protein Kinases; D014633:Valine