Ito Y, Sisido M, Imanishi Y
J Biomed Mater Res. 1986 Sep;20(7):1017-33. doi: 10.1002/jbm.820200715.
Novel polyetherurethaneureas containing tertiary amino groups in the side chains (PAEUU) were synthesized, quaternized with different alkyl halides (Q-PAEUU), and heparinized (H-PAEUU). The antithrombogenicity of PAEUU in vitro was improved by quaternization, and further by heparinization. The excellent antithrombogenicity of H-PAEUU was controlled by the kind of quaternizing agent through the polar effect of quaternizing agent on the water content and through the steric effect of quaternizing agent on the heparin content of H-PAEUU. The antithrombogenicity of H-PAEUU was found to be affected by the water content more strongly than by the heparin content. H-PAEUUs containing tertiary amino groups in the main chain, which were synthesized previously, showed a little better short-term antithrombogenicity than the present H-PAEUUs containing tertiary amino groups in the side chains. Since ammonium groups in the side chains of Q-PAEUU impose little steric hindrance against the heparin adsorption, the release of heparin from the side chains of H-PAEUU was slower but lasted longer than that from the main chain. Therefore, the present H-PAEUU is expected to be a long-term antithrombogenic material.
合成了侧链含有叔氨基的新型聚醚聚氨酯脲（PAEUU），用不同的卤代烷将其季铵化（Q-PAEUU），并进行肝素化处理（H-PAEUU）。PAEUU的体外抗血栓形成性通过季铵化得到改善，通过肝素化进一步改善。H-PAEUU优异的抗血栓形成性受季铵化剂种类的控制，这是通过季铵化剂对含水量的极性效应以及季铵化剂对H-PAEUU肝素含量的空间效应实现的。发现H-PAEUU的抗血栓形成性受含水量的影响比受肝素含量的影响更强。先前合成的主链含有叔氨基的H-PAEUUs的短期抗血栓形成性比目前侧链含有叔氨基的H-PAEUUs略好。由于Q-PAEUU侧链中的铵基团对肝素吸附几乎没有空间位阻，H-PAEUU侧链中肝素的释放比主链中慢但持续时间长。因此，目前的H-PAEUU有望成为一种长期抗血栓形成材料。
