（±）-1-酰基-3-（3,4-二氯苯基）-3-[2-（螺环取代的哌啶-1'-基）乙基]哌啶的合成及NK1受体拮抗活性
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.
作者信息
Kubota H, Okamoto Y, Fujii M, Ikeda K, Takeuchi M, Shibanuma T, Isomura Y
机构信息
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 1998 Jun 16;8(12):1541-6. doi: 10.1016/s0960-894x(98)00260-1.
(+/-)-1-Acyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines and their quaternary ammonium salts were prepared and evaluated for their NK1 receptor antagonistic activity. Some of these inhibited SP-induced contraction in guinea pig ileum with IC50 values at a level of 10(-9) M and showed potent inhibitory activity against selective NK1 receptor agonist-induced bronchoconstriction in guinea pigs.
制备了（±）-1-酰基-3-（3,4-二氯苯基）-3-[2-（螺环取代哌啶-1'-基）乙基]哌啶及其季铵盐，并对其NK1受体拮抗活性进行了评估。其中一些化合物在豚鼠回肠中抑制SP诱导的收缩，IC50值在10^(-9) M水平，并对豚鼠中选择性NK1受体激动剂诱导的支气管收缩显示出强效抑制活性。
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