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The glycine-prodrug, milacemide, increases the seizure threshold due to hyperbaric oxygen; prevention by 1-deprenyl.

作者信息

Youdim M B, Kerem D, Duvdevani Y

机构信息

Rappaport Family Research Institute, Faculty of Medicine, Technion, Haifa, Israel.

出版信息

Eur J Pharmacol. 1988 Jun 10;150(3):381-4. doi: 10.1016/0014-2999(88)90023-4.

DOI:10.1016/0014-2999(88)90023-4
PMID:3138141
Abstract

The novel glycine-prodrug anticonvulsant, milacemide (2-N-pentylaminoacetamide) (500 mg/kg), significantly increased (greater than 400% the seizure threshold induced by hyperbaric oxygen (4.5 atmosphere). This effect was significantly reduced by the selective inhibition of monoamine oxidase B by 1-deprenyl (2.0 mg/kg). 1-Deprenyl alone hardly affected the seizure threshold. These results suggest that, in the brain, milacemide is oxidized to glycine and that this reaction is mediated primarily by monoamine oxidase B. However, the interaction of milacemide metabolites (glycine amide, pentanoate and glycine) as antagonists of receptors of the glutamate NMDA (N-methyl-D-aspartate) subtype cannot be excluded.

摘要

相似文献

1
The glycine-prodrug, milacemide, increases the seizure threshold due to hyperbaric oxygen; prevention by 1-deprenyl.
Eur J Pharmacol. 1988 Jun 10;150(3):381-4. doi: 10.1016/0014-2999(88)90023-4.
2
Milacemide, a glycine pro-drug, inhibits strychnine-allodynia without affecting normal nociception in the rat.米拉美胺,一种甘氨酸前体药物,可抑制大鼠的士的宁诱导的异常性疼痛,而不影响正常痛觉。
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3
Effects of milacemide, a glycine prodrug, on ethanol's antiseizure efficacy.甘氨酸前体药物米那西胺对乙醇抗惊厥疗效的影响。
Pharmacol Biochem Behav. 1992 Feb;41(2):263-6. doi: 10.1016/0091-3057(92)90096-x.
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Effects of the glycine prodrug milacemide (2-N-pentylaminoacetamide) on catecholamine secretion from isolated adrenal medulla chromaffin cells.甘氨酸前体药物米拉醋胺(2-N-戊基氨基乙酰胺)对离体肾上腺髓质嗜铬细胞儿茶酚胺分泌的影响。
Br J Pharmacol. 1991 Nov;104(3):760-4. doi: 10.1111/j.1476-5381.1991.tb12501.x.
5
Milacemide, a glycine prodrug, enhances performance of learning tasks in normal and amnestic rodents.米拉美胺,一种甘氨酸前药,可提高正常和失忆啮齿动物的学习任务表现。
Pharmacol Biochem Behav. 1989 Dec;34(4):823-8. doi: 10.1016/0091-3057(89)90281-5.
6
Is the oxidation of milacemide by monoamine oxidase a major factor in its anticonvulsant actions?米那酰胺通过单胺氧化酶的氧化作用是其抗惊厥作用的主要因素吗?
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Microionophoretic study with milacemide, a glycine precursor, on mammalian central nervous system cells.使用甘氨酸前体米拉酰胺对哺乳动物中枢神经系统细胞进行微离子电泳研究。
Br J Pharmacol. 1990 May;100(1):119-25. doi: 10.1111/j.1476-5381.1990.tb12062.x.
8
Formation of the neurotransmitter glycine from the anticonvulsant milacemide is mediated by brain monoamine oxidase B.抗惊厥药米拉醋胺生成神经递质甘氨酸的过程由脑单胺氧化酶B介导。
J Neurochem. 1988 Apr;50(4):1011-6. doi: 10.1111/j.1471-4159.1988.tb10566.x.
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Antiepileptic drug pharmacokinetics and neuropharmacokinetics in individual rats by repetitive withdrawal of blood and cerebrospinal fluid: milacemide.通过反复采集血液和脑脊液研究米那西肽在大鼠个体中的抗癫痫药物药代动力学和神经药代动力学
Br J Pharmacol. 1993 Apr;108(4):1117-24. doi: 10.1111/j.1476-5381.1993.tb13514.x.
10
Does FAD-dependent polyamine oxidase contribute to the metabolism of milacemide?黄素腺嘌呤二核苷酸(FAD)依赖性多胺氧化酶是否参与米那普明的代谢?
J Neural Transm Suppl. 1990;32:351-6. doi: 10.1007/978-3-7091-9113-2_48.

引用本文的文献

1
Microionophoretic study with milacemide, a glycine precursor, on mammalian central nervous system cells.使用甘氨酸前体米拉酰胺对哺乳动物中枢神经系统细胞进行微离子电泳研究。
Br J Pharmacol. 1990 May;100(1):119-25. doi: 10.1111/j.1476-5381.1990.tb12062.x.
2
A review of the in vitro and in vivo neurochemical characterization of the NMDA/PCP/glycine/ion channel receptor macrocomplex.N-甲基-D-天冬氨酸/苯环己哌啶/甘氨酸/离子通道受体大复合物的体外和体内神经化学特征综述。
Neurochem Res. 1990 Feb;15(2):217-30. doi: 10.1007/BF00972212.
3
Effects of the glycine prodrug milacemide (2-N-pentylaminoacetamide) on catecholamine secretion from isolated adrenal medulla chromaffin cells.
甘氨酸前体药物米拉醋胺(2-N-戊基氨基乙酰胺)对离体肾上腺髓质嗜铬细胞儿茶酚胺分泌的影响。
Br J Pharmacol. 1991 Nov;104(3):760-4. doi: 10.1111/j.1476-5381.1991.tb12501.x.