Hsu K S, Lin-Shiau S Y
Institute of Pharmacology, College of Medicine, National Taiwan University, Taipei, R.O.C.
Neuropharmacology. 1993 Sep;32(9):877-83. doi: 10.1016/0028-3908(93)90143-q.
Potentiation by 4-phenylpyridine (a MAO-B inhibitor) on the neuromuscular blocking action of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) was studied in mouse phrenic nerve-diaphragm. MPTP blocked nerve-evoked twitches in a concentration (1-200 microM)-dependent manner. 4-Phenylpyridine, but not pargyline or tranylcypromine potentiated this inhibitory effect of MPTP. Pretreatment with 50 microM 4-phenylpyridine, reduced IC50 (concentration for 50% inhibition of twitch amplitude) values of MPTP from 53 to 18 microM and d-tubocurarine from 0.7 to 0.3 microM, respectively. 4-Phenylpyridine also enhanced the inhibitory action of MPTP and d-tubocurarine on acetylcholine (0.1 mM)-induced contracture of the denervated mouse diaphragm. The twitch inhibition induced by alpha-bungarotoxin and the specific binding of [125I]alpha-bungarotoxin to the mouse diaphragm were potentiated by 4-phenylpyridine but the inhibitory action of MPTP and d-tubocurarine on [125I]alpha-bungarotoxin binding were not significantly changed by pretreatment with 4-phenylpyridine. Electrophysiological studies revealed that the inhibitory actions of MPTP and d-tubocurarine on the amplitudes of m.e.p.ps and e.p.ps were augmented by 4-phenylpyridine. These indicate that 4-phenylpyridine enhanced the neuromuscular blocking action of the MPTP and d-tubocurarine at the postsynaptic nicotinic acetylcholine receptors. The implication of this finding is that the possible application of 4-phenylpyridine in the MPTP-induced Parkinson's disease is limited by its potentiation on the neuromuscular blocking action of MPTP.
在小鼠膈神经-膈肌标本上研究了4-苯基吡啶(一种单胺氧化酶B抑制剂)对1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)神经肌肉阻滞作用的增强效应。MPTP以浓度(1-200微摩尔)依赖性方式阻断神经诱发的抽搐。4-苯基吡啶可增强MPTP的这种抑制作用,而帕吉林或反苯环丙胺则无此作用。用50微摩尔4-苯基吡啶预处理后,MPTP的IC50(抑制抽搐幅度50%的浓度)值从53微摩尔降至18微摩尔,d-筒箭毒碱的IC50值从0.7微摩尔降至0.3微摩尔。4-苯基吡啶还增强了MPTP和d-筒箭毒碱对乙酰胆碱(0.1毫摩尔)诱导的去神经小鼠膈肌挛缩的抑制作用。4-苯基吡啶可增强α-银环蛇毒素诱导的抽搐抑制作用以及[125I]α-银环蛇毒素与小鼠膈肌的特异性结合,但4-苯基吡啶预处理并未显著改变MPTP和d-筒箭毒碱对[125I]α-银环蛇毒素结合的抑制作用。电生理研究表明,4-苯基吡啶增强了MPTP和d-筒箭毒碱对微小终板电位和终板电位幅度的抑制作用。这些结果表明,4-苯基吡啶在突触后烟碱型乙酰胆碱受体处增强了MPTP和d-筒箭毒碱的神经肌肉阻滞作用。这一发现的意义在于,4-苯基吡啶对MPTP神经肌肉阻滞作用的增强可能限制了其在MPTP诱导的帕金森病中的潜在应用。