一类新型的基于二胺的人组胺H3受体拮抗剂：4-（氨基烷氧基）苄胺。
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
作者信息
Apodaca Richard, Dvorak Curt A, Xiao Wei, Barbier Ann J, Boggs Jamin D, Wilson Sandy J, Lovenberg Timothy W, Carruthers Nicholas I
机构信息
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, California 92121, USA.
出版信息
J Med Chem. 2003 Aug 28;46(18):3938-44. doi: 10.1021/jm030185v.
4-(Aminoalkoxy)benzylamines were prepared and screened for in vitro activity at the human histamine H(3) receptor. Some members of this series exhibited subnanomolar binding affinities. Analogues in which one nitrogen atom was replaced with a methine group showed greatly reduced binding affinities. Six members of this series were found to be antagonists in a cell-based model of human histamine H(3) receptor activation. One member of this series, 1-[4-(3-piperidin-1-ylpropoxy)benzyl]piperidine (7b), was found to be a selective and potent human H(3) receptor antagonist.
制备了4-(氨基烷氧基)苄胺，并对其在人组胺H(3)受体上的体外活性进行了筛选。该系列中的一些成员表现出亚纳摩尔级的结合亲和力。其中一个氮原子被次甲基取代的类似物显示出结合亲和力大大降低。在基于细胞的人组胺H(3)受体激活模型中，发现该系列的六个成员为拮抗剂。该系列的一个成员，1-[4-(3-哌啶-1-基丙氧基)苄基]哌啶(7b)，被发现是一种选择性强效的人H(3)受体拮抗剂。
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