Effects of natural pyrimidines and of certain related compounds on the spontaneous activity of the mouse.
Effects of natural pyrimidines and of certain related compounds on the spontaneous activity of the mouse.
复制标题
天然嘧啶和某些相关化合物对小鼠自发活动的影响。
DOI：
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发表时间：
1978
影响因子：
3.5
通讯作者：
G. Lam
中科院分区：
文献类型：
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作者：
R. S. Krooth;W. Hsiao;G. Lam
尿嘧啶和其他天然嘧啶类药物可能影响哺乳动物脑的唤醒水平，因为：1）类似尿嘧啶的六元杂环构成许多催眠药结构的一部分;和2）6-氮尿嘧啶尿苷（及其核苷）已显示对包括人在内的几种哺乳动物具有催眠作用。尿苷，6-氮杂尿苷，胞苷或胸苷抑制成年雄性C-57小鼠的自发活动。6-氮尿苷的效力远低于其他测试的核苷。胞嘧啶、巴比妥酸、2-硫代巴比妥酸、2，4-二羟基吡啶及多种嘧啶类催化剂对活性无影响。胸腺嘧啶、尿嘧啶、6-氮尿嘧啶、巴比妥和苯巴比妥在较低剂量下增加活性，在较高剂量下降低活性。6-氮尿嘧啶和尿嘧啶作为活性刺激物的效力大致相同，但6-氮尿嘧啶作为活性刺激物的效力约为尿嘧啶的两倍。胸腺嘧啶比尿嘧啶更有活性，无论是作为兴奋剂还是作为兴奋剂，其效力都只有巴比妥的10%。对于胸腺嘧啶和两种巴比妥酸盐，ED 50（抑制活动）与LD 50相同，而引起50%活动刺激的剂量比LD 50小一个数量级。这些结果提示巴比妥类药物可能通过模拟某些受体上胸腺嘧啶或尿嘧啶的结构而影响觉醒。
Uracil and perhaps other natural pyrimidines may effect the level of arousal of the mammalian brain since: 1) heterocyclic 6-membered rings, which resemble uracil, form part of the structure of many hypnotics; and 2) 6-azauracil (and its riboside) have shown to be hypnotic for several mammalian species, including man. The parenteral administration of uridine, 6-azauridine, cytidine or thymidine depressed the spontaneous activity of adult male C-57 mice. 6-Azauridine was much less potent than the other ribosides tested. Cytosine, barbituric acid, 2-thiobarbituric acid, 2,4-dihydroxypyridine and a variety of pyrimidine catabolites had no effect on activity. Thymine, uracil, 6-azauracil, barbital and phenobarbital increased activity at lower doses and decreased activity at higher ones. 6-Azauracil and uracil were about equally potent as stimulants of activity, but 6-azauracil had about twice the potency of uracil as a depressant of activity. Thymine, which was more active than uracil, had about 10% the potency of barbital, both as a stimulant and as a depressant of activity. For thymine and the two barbiturates the ED50 (for depression of activity) was of the same magnitude as the LD50, while the dose which caused 50% stimulation of activity was about an order of magnitude less than the LD50. These results suggest that the barbiturates might affect arousal by simulating the structure of thymine or uracil at some receptor.