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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Structure-activity relationship on (+/-)-nantenine derivatives in antiserotonergic activities in rat aorta.
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Structure-activity relationship on (+/-)-nantenine derivatives in antiserotonergic activities in rat aorta.

机译：大鼠主动脉抗5-羟色胺活性中（+/-）-南宁衍生物的构效关系。

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摘要

A series of nine (+/-)-nantenine derivatives were synthesized and assayed for their pharmacological activities by using tension in aorta and binding experiments in rat brain membrane. Replacing a methyl group with a hydrogen ((+/-)-nornantenine) and an ethyl group at a nitrogen atom ((+/-)-ethylnornantenine) or introducing a hydroxyl group at the alpha/beta position of C-4 or displacement of a methoxy moiety at the C-1 position with a hydroxyl ((+/-)-domesticine) of (+/-)-nantenine decreased the affinity. Moreover, changing a methyl group of (+/-)-domesticine to hydrogen at a nitrogen atom ((+/-)-nordomesticine) caused loss of the activities. These results suggest that a methyl group at a nitrogen atom and a methoxy moiety at C-1 play important roles in the development of the antiserotonergic activity. Molecular modeling analysis of the interaction between the 5-HT2A receptor and (+/-)-nantenine suggested that electron lone pairs of N-6 and of the oxygen atom of the methoxy group at C-1 are important in forming a hydrogen bond to Asp155 and Asn343 of the 5-HT2A receptor, respectively.
机译：通过使用主动脉中的张力和大鼠脑膜中的结合实验，合成了一系列九种（+/-）-南丁宁衍生物，并对其药理活性进行了测定。在氢原子（（+/-）-乙基降冰片烯）上用氢（（+/-）-降冰片烯）和乙基取代甲基或在C-4的α/β位置或取代处引入羟基在C-1位置的甲氧基部分与（+/-）-南丁氨酸的羟基（（+/-）-苯丁胺）的亲和力降低。此外，在氮原子（（+/-）-nordomesticine）上将（+/-）-domesticine的甲基改变为氢导致活性丧失。这些结果表明，氮原子上的甲基和C-1上的甲氧基部分在抗5-羟色胺活性的发展中起重要作用。对5-HT2A受体和（+/-）-南丁烯之间相互作用的分子模型分析表明，N-6的电子孤对和C-1处甲氧基的氧原子对形成氢键很重要。 5-HT2A受体的Asp155和Asn343。

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