体外活性
Pretreatment with 50 mM 4-phenylpyridine, reduces IC50 (concentration for 50% inhibition of twitch amplitude) values of MPTP from 53 to 18 mM and d-tubocurarine from 0.7 to 0.3 mM, respectively, in mouse phrenic nerve-diaphragm[3].
体内活性
The toxic effect of MPTP can be completely abolished in vivo by treatment with a monoamine oxidase inhibitor and potentiated by an inhibitor of catechol-O-methyltransferase[1]. Allopurinol potentiated the MPTP (35 mg/kg)-induced decrease in the DOPAC+HVA/DA ratio and increase in striatal AA oxidation of the rat[2]. Gas1 expressions are significantly elevated in the majority of the reactive astrocytes of the brains with LPS or MPTP insults in animal models[4].
参考文献
[1]Desole M S, et al. Further investigation of allopurinol effects on MPTP-induced oxidative stress in the striatum and brain stem of the rat. Source:Pharmacol.Biochem.Behav., 1996, 54, No. 2, 377-83. [2]Langston J W, Irwin I. MPTP Neurotoxicity: An Overview and Characterization of Phases of Toxicity. II. Selective Accumulation of MPP in the Substantia Nigra: A Key to Neurotoxicity (Question). Life Sci., 1985, 36, No. 3, 201-12. [3]Sun XL, et al. Gas1 up-regulation is inducible and contributes to cell apoptosis in reactive astrocytes in the substantia nigra of LPS and MPTP models. J Neuroinflammation. 2016 Jul 8;13(1):180. [4]Hsu K S, et al. Potentiation of MPTP by 4-Phenylpyridine on the Neuromuscular Blockade in Mouse Phrenic Nerve-Diaphragm. Neuropharmacology, 1993, 32, No. 9, 877-83.