Schunack W, Stark H
Freie Universität Berlin, Institute of Pharmacy, Germany.
Eur J Drug Metab Pharmacokinet. 1994 Jul-Sep;19(3):173-8. doi: 10.1007/BF03188918.
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs of the primary amine with benzophenone derivatives. In the antagonist field a number of new leads belonging to different chemical classes are discovered. Potential compounds for drug development are identified. The radiolabelled probe [125I]iodoproxyfan shows high potency and selectivity in functional and binding studies. It is a useful compound for binding assays as well as for the detection and localization of histamine H3-receptors.
本文综述了用于组胺H3受体特性表征的高效选择性配体的研究进展。在激动剂领域，发现天然配体的立体选择性甲基化衍生物具有所需的药效学性质。通过用二苯甲酮衍生物形成伯胺的生物可逆偶氮甲碱前药，可以改善药代动力学性质。在拮抗剂领域，发现了许多属于不同化学类别的新先导化合物。确定了潜在的药物开发化合物。放射性标记探针[125I]碘普罗番在功能和结合研究中显示出高效性和选择性。它是一种用于结合测定以及组胺H3受体检测和定位的有用化合物。
