Brandes L J, Bogdanovic R P, Cawker M D, Bose R
Cancer Chemother Pharmacol. 1986;18(1):21-3. doi: 10.1007/BF00253057.
N,N-diethyl-2-[(4-phenylmethyl)-phenoxy]-ethanamine HCl (DPPE), a novel histamine antagonist (?H3), which selectively binds with high affinity to the antiestrogen-binding site (AEBS/?H3), inhibits the activity of calmodulin-dependent myosin light chain kinase (MLCK) only at concentrations greater than 1 mM, as opposed to tamoxifen (TAM), which has an IC50 = 4 microM in the same assay. This suggests that the antiestrogen-binding site is distinct from the site on calmodulin which binds TAM and phenothiazines. However, at an in vitro concentration of 1 X 10(-6) M, the antiproliferative effects of DPPE and several phenothiazines, which also compete for binding to AEBS/?H3, are about equal; this suggests that affinity for AEBS/?H3 rather than that for the calmodulin-binding site may correlate with clinically relevant antigrowth effects of these compounds.
N,N - 二乙基 - 2 - [(4 - 苯甲基) - 苯氧基] - 乙胺盐酸盐（DPPE）是一种新型组胺拮抗剂（H3），它以高亲和力选择性地与抗雌激素结合位点（AEBS/H3）结合，仅在浓度大于1 mM时才抑制钙调蛋白依赖性肌球蛋白轻链激酶（MLCK）的活性，而他莫昔芬（TAM）在相同测定中IC50 = 4 microM。这表明抗雌激素结合位点与钙调蛋白上结合TAM和吩噻嗪的位点不同。然而，在体外浓度为1×10(-6) M时，DPPE和几种也竞争与AEBS/H3结合的吩噻嗪的抗增殖作用大致相等；这表明对AEBS/H3的亲和力而非对钙调蛋白结合位点的亲和力可能与这些化合物临床上相关的抗生长作用相关。
