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米那普明在大鼠体内的单胺氧化酶抑制特性

Monoamine oxidase inhibitory properties of milacemide in rats.

作者信息

Truong D D, Diamond B, Pezzoli G, Mena M A, Fahn S

机构信息

Department of Neurology, Columbia University College of Physicians and Surgeons, New York, N.Y. 10032.

出版信息

Life Sci. 1989;44(15):1059-66. doi: 10.1016/0024-3205(89)90558-4.

DOI:10.1016/0024-3205(89)90558-4
PMID:2784529
Abstract

Milacemide is a glycine prodrug with reported antiepileptic antimyoclonic properties. In this study, milacemide increased "wet dog shakes" in rats pretreated with 5-Hydroxytryptophan (5-HTP) and carbidopa. Moreover, it worsened the serotonin behavior syndrome precipitated by 5-HTP and the monoamine oxidase inhibitor tranylcypromine. The serotonin syndrome was also elicited by the combination of milacemide and 5-HTP without tranylcypromine. In vitro, milacemide inhibited both monoamine oxidase A and B from the frontal cortex of rats, to a greater extent for MAO B. This drug is currently under investigation in humans as an antiepileptic agent and precautions for the consequences of monoamine oxidase inhibition should be considered when the drug is used in high doses.

摘要

米拉醋胺是一种具有抗癫痫和抗肌阵挛特性报道的甘氨酸前体药物。在本研究中,米拉醋胺增加了用5-羟色氨酸(5-HTP)和卡比多巴预处理的大鼠的“湿狗样抖动”。此外,它还加重了由5-HTP和单胺氧化酶抑制剂反苯环丙胺引发的血清素行为综合征。血清素综合征也可由米拉醋胺和5-HTP联合使用(无反苯环丙胺)引发。在体外,米拉醋胺抑制大鼠额叶皮质中的单胺氧化酶A和B,对MAO B的抑制作用更大。该药物目前正在作为抗癫痫药物进行人体研究,当高剂量使用该药物时,应考虑单胺氧化酶抑制后果的预防措施。

相似文献

1
Monoamine oxidase inhibitory properties of milacemide in rats.米那普明在大鼠体内的单胺氧化酶抑制特性
Life Sci. 1989;44(15):1059-66. doi: 10.1016/0024-3205(89)90558-4.
2
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.
3
The novel neuropsychotropic agent milacemide is a specific enzyme-activated inhibitor of brain monoamine oxidase B.新型神经精神药物米拉醋胺是一种脑单胺氧化酶B的特异性酶激活抑制剂。
J Neurochem. 1989 Oct;53(4):1109-16. doi: 10.1111/j.1471-4159.1989.tb07403.x.
4
Effect of milacemide on extracellular and tissue concentrations of dopamine and 5-hydroxytryptamine in rat frontal cortex.米拉美胺对大鼠额叶皮质中多巴胺和5-羟色胺细胞外及组织浓度的影响。
Br J Pharmacol. 1992 Jan;105(1):59-62. doi: 10.1111/j.1476-5381.1992.tb14210.x.
5
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?
Biochem Pharmacol. 1991 Jun 1;41(11):1731-7. doi: 10.1016/0006-2952(91)90177-7.
6
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.
7
MAO activity, metabolism and anticonvulsant activity of milacemide in rats and mice.米那西肽在大鼠和小鼠体内的单胺氧化酶活性、代谢及抗惊厥活性
J Neural Transm Suppl. 1990;32:123-9. doi: 10.1007/978-3-7091-9113-2_17.
8
Species differences in the interactions of the anticonvulsant milacemide and some analogues with monoamine oxidase-B.抗惊厥药米拉醋胺及一些类似物与单胺氧化酶-B相互作用的种属差异
Biochem Pharmacol. 1995 Jul 31;50(3):317-24. doi: 10.1016/0006-2952(95)00145-p.
9
Interactions of some analogues of the anticonvulsant milacemide with monoamine oxidase.抗惊厥药米拉醋胺的某些类似物与单胺氧化酶的相互作用。
Biochem Pharmacol. 1994 Aug 30;48(5):905-14. doi: 10.1016/0006-2952(94)90361-1.
10
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。
Pain. 1998 Jul;77(1):87-95. doi: 10.1016/S0304-3959(98)00086-4.

引用本文的文献

1
Effect of milacemide on extracellular and tissue concentrations of dopamine and 5-hydroxytryptamine in rat frontal cortex.米拉美胺对大鼠额叶皮质中多巴胺和5-羟色胺细胞外及组织浓度的影响。
Br J Pharmacol. 1992 Jan;105(1):59-62. doi: 10.1111/j.1476-5381.1992.tb14210.x.