The inhibition of human platelet 5‐hydroxytryptamine uptake by tricyclic antidepressive drugs. The relation between structure and potency
The inhibition of human platelet 5‐hydroxytryptamine uptake by tricyclic antidepressive drugs. The relation between structure and potency
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三环类抗抑郁药物对人血小板 5-羟色胺摄取的抑制结构与效力之间的关系。
DOI：
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发表时间：
1969
期刊：
影响因子：
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通讯作者：
A. C. Tait
中科院分区：
文献类型：
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作者：
A. Todrick;A. C. Tait
研究了与抗抑郁药物丙咪嗪相关的35个化合物的化学结构，研究了它们在体外抑制人血小板摄取5-羟色胺的能力。用苯环上2或3位的小分子正电基团取代，得到的化合物比原型化合物更有活性，3-氯丙咪胺在本试验中的效力是原型的五倍。抗抑郁药物的特征七元环的改变降低了活性，而碱性侧链上的取代则破坏了活性。叔胺比它们的脱甲基衍生物具有更强的抑制作用。在这种和其他方面，抑制人血血小板摄取5-羟色胺的活性结构与抑制大鼠心脏摄取去甲肾上腺素的活性结构不同。
Thirty‐five compounds related to the antidepressive drug imipramine in chemical structure have been examined for their capacity to inhibit the uptake of 5‐hydroxytryptamine by human platelets in vitro. Substitution by small‐sized electropositive groups in positions 2 or 3 of a benzene ring gave compounds more active than the prototype, 3‐chloroimipramine being five times as potent on this test. Alteration of the characteristic seven‐membered ring of the antidepressive drugs reduced the activity while substitution in the basic side‐chain destroyed it. The tertiary amines were more potent inhibitors than their demethylated derivatives. In this and other ways the active structure for the inhibition of 5‐ht uptake by human blood platelets differs from that for the inhibition of noradrenaline uptake by the rat heart.