EVIDENCE THAT THE ANTIESTROGEN BINDING-SITE IS A HISTAMINE OR HISTAMINE-LIKE RECEPTOR
EVIDENCE THAT THE ANTIESTROGEN BINDING-SITE IS A HISTAMINE OR HISTAMINE-LIKE RECEPTOR
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DOI：
10.1016/0006-291x(85)90271-2
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发表时间：
1985-01-01
影响因子：
3.1
通讯作者：
MACDONALD, LM
中科院分区：
文献类型：
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作者：
BRANDES, LJ;MACDONALD, LM
N，N-二乙基-2-[（4-苯基甲基）-苯氧基]-乙胺盐酸盐（DPPE）是一种对抗雌激素结合位点具有选择性的化合物，其结构类似于抗组胺药的氨基乙基醚基团。显然，H1-拮抗剂而不是H2-拮抗剂也按以下顺序竞争该位点：DPPE =羟嗪=高氯酸嗪>苯妥沙明>吡拉明>苯海拉明。这些化合物对抗雌激素结合位点的亲和力与它们对MCF-7和EVSA-T人乳腺癌细胞的体外细胞毒性相关。他莫昔芬、DPPE和羟嗪也与毛地黄皂苷溶解的大鼠肝微粒体中存在的H1受体结合，但亲和力低于对该位点具有选择性的吡拉明;本制剂中H1与抗雌激素结合位点的比例为4：1。抗雌激素结合位点可以全部或部分是不同于H1和H2的组胺受体。
N,N-diethyl-2-[(4-phenylmethyl)-phenoxy]-ethanamine.cntdot.HCl(DPPE), a compound selective for the antiestrogen binding site, is structurally similar to the aminoethyl ether group of antihistamines. H1-, but not H2-antagonists, apparently, also compete for this site in the order; DPPE = hydroxyzine = perchlorperazine > phenyltoloxamine > pyrilamine > diphenhydramine. The affinity of these compounds for the antiestrogen binding site correlates with their in vitro cytotoxicity against MCF-7 and EVSA-T human breast cancer cells. Tamoxifen, DPPE and hydroxyzine also bind to H1 receptors present in digitonin-solubilized rat liver microsomes, but with less affinity than pyrilamine, which is selective for this site; the ratio of H1 to antiestrogen binding sites in this preparation is 4:1. The antiestrogen binding site may be, in whole or in part, a receptor for histamine different from H1 and H2.