Muramatsu M, Kuriyama K
Jpn J Pharmacol. 1976 Apr;26(2):249-54. doi: 10.1254/jjp.26.249.
Effects of parathion and di-isopropyl fluorophosphate (DFP) on acetylcholine (ACh) synthesis in the mouse brain were investigated. In addition to well known cholinesterase (ChE) inhibition, parathion showed inhibitory effects on the activity of synaptosomal choline acetyltransferase (ChAc), and on the uptake of [14C-methyl]-choline and ACHh synthesis in subcellular fractions of the brain. DFP inhibited ChE activity, but had no significant effects on the choline uptake and ACh synthesis per se. Possible significance of these findings in the pharmacological actions of organophosphorus compounds is briefly discussed.
研究了对硫磷和二异丙基氟磷酸酯(DFP)对小鼠脑内乙酰胆碱(ACh)合成的影响。除了众所周知的胆碱酯酶(ChE)抑制作用外,对硫磷还对突触体胆碱乙酰转移酶(ChAc)的活性、[14C-甲基]胆碱的摄取以及脑亚细胞组分中的ACh合成表现出抑制作用。DFP抑制ChE活性,但对胆碱摄取和ACh合成本身没有显著影响。简要讨论了这些发现对有机磷化合物药理作用的可能意义。