TRICYCLIC ANALOGS OF MELATONIN
TRICYCLIC ANALOGS OF MELATONIN
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DOI：
10.1021/jm00304a017
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发表时间：
1969-01-01
影响因子：
7.3
通讯作者：
WITKOP, B
中科院分区：
文献类型：
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作者：
KOBAYASHI, T;SPANDE, TF;WITKOP, B
褪黑激素的角三环类似物，8-甲氧基-6-氧代-3，4，6，7-四氢-1H，5 H-氮杂辛[4，5，6-cd]吲哚（IV）以及线性“脱氢褪黑激素”，即，5-甲氧基-1-乙酰基-2，3-二氢吡咯并[2，3-b]吲哚（VI）仅保留褪黑激素活性的极小部分。内酰胺IV和相应的胺V对小鼠和猫的中枢神经系统无明显影响。褪黑激素，N-乙酰基-5-甲氧基色胺（I），2已从松果体提取物中分离出来，并在哺乳动物和人的外周神经中鉴定。3它的生物学特性不同于其他已知的增白剂。4我们现在已经应用了X-的光环化，
The angular tricyclic analog of melatonin, 8-methoxy-6-oxo-3, 4, 6, 7-tetrahydro-lH, 5H-azocin [4, 5, 6-cd] indole (IV) as well as the linear “dehydromelatonin,’’viz., 5-methoxy-l-acetyl-2, 3-dihydropyrrolo [2, 3-6] indole (VI) had retained only tiny fractions of the activity of melatonin. The lactam IV and the corresponding amine V showed no major CNS effects in mice andcats.Melatonin, N-acetyl-5-methoxytryptamine (I), 2 has been isolated from extracts of pineal glands and identi-fied in peripheral nerves of mammals and man. It· is conveniently assayed by its lightening effect on frog melanocytes. 3 Its biological properties are different from those of other known lightening agents. 4 We have now applied the photocyclization of X-