Łazewska Dorota, Kuder Kamil, Ligneau Xavier, Schwartz Jean-Charles, Schunack Walter, Stark Holger, Kieć-Kononowicz Katarzyna
Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Kraków, Poland.
Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. doi: 10.1016/j.bmc.2008.07.071. Epub 2008 Jul 29.
Synthesis and biological evaluation of the novel histamine H(3) receptor ligands is described. Two series of ethers (aliphatic and aromatic) have been prepared by four different methods. Compounds were evaluated for their affinities at recombinant human H(3) receptor stably expressed in CHO cells. The ethers show from low to moderate in vitro affinities in nanomolar concentration range. The most potent compound was the 1-[3-(4-tert-butylphenoxy)propyl]-4-piperidino-piperidine 16 (hH(3)R K(i)=100 nM). Several members of the new series investigated under in vivo conditions, proved to be inactive.
描述了新型组胺H(3)受体配体的合成及生物学评价。通过四种不同方法制备了两个系列的醚（脂肪族和芳香族）。评估了这些化合物对稳定表达于CHO细胞中的重组人H(3)受体的亲和力。这些醚在纳摩尔浓度范围内表现出低至中等的体外亲和力。最有效的化合物是1-[3-(4-叔丁基苯氧基)丙基]-4-哌啶基哌啶16（hH(3)R K(i)=100 nM）。在体内条件下研究的新系列中的几个成员被证明无活性。
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