Ethylcholine mustard aziridinium blocks the axoplasmic transport of acetylcholinesterase in cholinergic nerve fibres of the rat.
A cholinotoxin, ethylcholine mustard aziridinium ion, (AF64A) specifically and irreversibly blocks the intraaxonal transport of acetylcholinesterase in the rat. Impairment of the transport of this enzyme in the septo-hippocampal cholinergic fibres and in the sciatic nerve has been studied, using different doses of AF64A. It is demonstrated that the effect on the axonal transport is dose-dependent, but is not related to the mode of drug application. AF64A thus may exert its neurotoxic effects on cholinergic neurons at several target sites of action. In addition to the localized presynaptic mechanisms, it may also be compromising cholinergic function by inhibiting axonal transport in vivo.
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Kása
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Hanin
D000818:Animals; D001370:Axonal Transport / Q000187:drug effects; D001388:Aziridines / Q000494:pharmacology*; D001389:Azirines / Q000494:pharmacology*; D001693:Biological Transport, Active / Q000187:drug effects; D002794:Choline / Q000031:analogs & derivatives* / Q000494:pharmacology; D002799:Cholinergic Fibers / Q000187:drug effects / Q000201:enzymology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D006624:Hippocampus / Q000201:enzymology; D006651:Histocytochemistry; D009466:Neuromuscular Blocking Agents / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D012584:Sciatic Nerve / Q000201:enzymology
D001388:Aziridines; D001389:Azirines; D002800:Cholinesterase Inhibitors; D009466:Neuromuscular Blocking Agents; C044894:ethylcholine aziridinium; D002794:Choline