苯甲脒衍生物对豚鼠补体的抑制作用。I. 间-（间苯氧基丙氧基）苯甲脒的对硝基苯脲衍生物对豚鼠补体成分溶血活性的影响。

Inhibition of guinea-pig complement by derivatives of benzamidine. I. Effect of p-nitrophenylureido derivative of m-(m-phenoxypropoxy)benzamidine on guinea-pig complement component haemolytic activity.

作者信息

Glovsky M M, Cory M, Alenty A

出版信息

Immunology. 1974 Apr;26(4):819-29.

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1423170/

Abstract

Derivatives of benzamidine have been shown to be potent inhibitors of whole guinea-pig complement. Among these compounds the -[-(-nitrophenylureido) phenoxypropoxy] benzamidine (NPUPPB) was the most potent complement inhibitor synthesized. NPUPPB blocked the addition of C1 to EAC4. It had no effect on the stability of EAC4 or the decay rate of EAC42. It also blocked the addition of C2 to EAC14. No effect of the inhibitor was found when C3 was added to EAC142. A profound inhibition occurred when either C[unk]567 was added to EAC1423 or when C5 was added to EAC1423. A slight though possibly insignificant effect occurred when C6 or C7 were added to EAC4235 and EAC42356. No effect occurred when C8 and C9 were added to the heat-stable intermediate EAC43567. NPUPPB is a potent though poorly soluble competitive inhibitor of complement activity.

摘要

苯甲脒衍生物已被证明是豚鼠全补体的有效抑制剂。在这些化合物中，-[-(-硝基苯脲基)苯氧基丙氧基]苯甲脒（NPUPPB）是合成的最有效的补体抑制剂。NPUPPB阻断了C1与EAC4的结合。它对EAC4的稳定性或EAC42的衰变率没有影响。它还阻断了C2与EAC14的结合。当将C3添加到EAC142时，未发现该抑制剂有作用。当将C[unk]567添加到EAC1423或将C5添加到EAC1423时，会发生显著抑制。当将C6或C7添加到EAC4235和EAC42356时，会产生轻微但可能不显著的作用。当将C8和C9添加到热稳定中间体EAC43567时，没有作用。NPUPPB是一种有效的补体活性竞争性抑制剂，尽管其溶解性较差。

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