吗氯贝胺是否像其他选择性单胺氧化酶-A抑制剂一样刺激褪黑素的合成？
Does moclobemide stimulate melatonin synthesis as the other selective MAO-A inhibitors do?
作者信息
Oxenkrug G F, Requintina P J, Yuwiler A
机构信息
Brown University, VAMC, Providence, Rhode Island.
出版信息
J Neural Transm Suppl. 1990;32:171-5. doi: 10.1007/978-3-7091-9113-2_25.
It has been reported that selective MAO-A inhibitors, clorgyline and brofaromine, but not the MAO-B inhibitors, deprenyl and pargyline, stimulated rat pineal melatonin synthesis in humans and animals. Recent studies, however, found no effect of moclobemide, a selective MAO-A inhibitor, on human plasma melatonin levels. Present study found that in vitro moclobemide produced very weak stimulation of rat pineal NAT activity. However, in vivo moclobemide induced a significant increase of rat pineal NAS and melatonin content, and a dramatic decrease of 5-HIAA content (HPLC-fluorimetric procedure). Moclobemide's effect on melatonin and related indoles could be detected as early as 30 min after the injection and lasted, at least, for 2 h. The possible reasons for discrepancies between human and animal data are discussed.
据报道，选择性单胺氧化酶-A抑制剂氯吉兰和溴法罗明可刺激人和动物的大鼠松果体褪黑素合成，但单胺氧化酶-B抑制剂司立吉林和帕吉林则无此作用。然而，最近的研究发现，选择性单胺氧化酶-A抑制剂吗氯贝胺对人体血浆褪黑素水平没有影响。目前的研究发现，体外实验中吗氯贝胺对大鼠松果体N-乙酰基转移酶（NAT）活性的刺激作用非常微弱。然而，在体内实验中，吗氯贝胺可使大鼠松果体N-乙酰基色胺（NAS）和褪黑素含量显著增加，5-羟吲哚乙酸（5-HIAA）含量显著降低（采用高效液相色谱-荧光检测法）。吗氯贝胺对褪黑素及相关吲哚的作用在注射后30分钟即可检测到，至少持续2小时。文中讨论了人和动物数据存在差异的可能原因。
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