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已经证明芳香哌嗪类化合物能与5-羟色胺5-HT_(1A)和5-HT_(1B)受体结合。为设计新的5-HT_(1A)激动剂和拮抗剂,作者先排除那些与5-HT_(1B)活性关系密切的结构特点,然后设计并筛选出一些与5-HT_(1A)亲和力高的化合物。其中NAN-190既无1-(3-三氟甲苯基)哌嗪样激动作用又无拮抗1-(3-三氟甲苯基)哌嗪的作用,但具有能拮抗5-HT_(1A)激动剂8-羟基-2-(双-正丙氨基)-1,2,3,4-四氢化萘的作用,提示NAN-190可能是一个潜在的5-HT_(1A)拮抗剂。
Aromatic piperazines have been shown to bind to serotonin 5-HT 1A and 5-HT 1B receptors. To design novel 5-HT 1A agonists and antagonists, the authors first excluded those structural features closely related to 5-HT 1B activity and then designed and screened some of the 5-HT 1A -dependent Compound. Among them, NAN-190 had neither 1- (3-trifluoromethylphenyl) piperazine-like agonism nor antagonism of 1- (3-trifluoromethylphenyl) piperazine but antagonized 5-HT 1A agonism The effect of 8-hydroxy-2- (bis-n-propylamino) -1,2,3,4-tetrahydronaphthalene suggests that NAN-190 may be a potential antagonist of 5-HT 1A.