Truong D D, Diamond B, Pezzoli G, Mena M A, Fahn S
Department of Neurology, Columbia University College of Physicians and Surgeons, New York, N.Y. 10032.
Life Sci. 1989;44(15):1059-66. doi: 10.1016/0024-3205(89)90558-4.
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.
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。