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新型查尔酮类荧光人组氨酸 h(3)受体配体作为药理学工具。

Novel chalcone-based fluorescent human histamine h(3) receptor ligands as pharmacological tools.

机构信息

ZAFES/CMP/ICNF, Biocenter, Institute of Pharmaceutical ChemistryJohann Wolfgang Goethe University Frankfurt am Main, Germany.

出版信息

Front Syst Neurosci. 2012 Mar 26;6:14. doi: 10.3389/fnsys.2012.00014. eCollection 2012.

DOI:10.3389/fnsys.2012.00014
PMID:22470321
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3312100/
Abstract

Novel fluorescent chalcone-based ligands at human histamine H(3) receptors (hH(3)R) have been designed, synthesized, and characterized. Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif. Tetralones as chemical precursors and related fluorescent chalcones exhibit affinities at hH(3)R in the same concentration range like the reference antagonist ciproxifan (hH(3)R pK(i) value of 7.2). Fluorescence characterization of our novel ligands shows emission maxima about 570 nm for yellow fluorescent chalcones and ≥600 nm for the red fluorescent derivatives. Interferences to cellular autofluorescence could be excluded. All synthesized chalcone compounds could be used to visualize hH(3)R proteins in stably transfected HEK-293 cells using confocal laser scanning fluorescence microscopy. These novel fluorescent ligands possess high potential to be used as pharmacological tools for hH(3)R visualization in different tissues.

摘要

新型荧光查耳酮类化合物作为人源组胺 H3 受体 (hH3R) 的配体被设计、合成和鉴定。所描述的化合物是非咪唑类西替利嗪类似物，具有四氢萘酮结构。四氢萘酮作为化学前体和相关的荧光查尔酮在 hH3R 上具有与参考拮抗剂西替利嗪 (hH3R pK(i) 值为 7.2) 相同的浓度范围的亲和力。我们新型配体的荧光特性显示，黄色荧光查尔酮的发射最大值约为 570nm，而红色荧光衍生物的发射最大值大于 600nm。可以排除细胞自发荧光的干扰。所有合成的查尔酮化合物都可以使用共聚焦激光扫描荧光显微镜，在稳定转染的 HEK-293 细胞中用于可视化 hH3R 蛋白。这些新型荧光配体具有作为 hH3R 可视化的药理学工具在不同组织中应用的巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/c002fe0c0b6d/fnsys-06-00014-a004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/8ed4a912277c/fnsys-06-00014-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/81c4e87b7377/fnsys-06-00014-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/0a264b9e48ef/fnsys-06-00014-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/c075fdbf8588/fnsys-06-00014-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/aff3ac50725c/fnsys-06-00014-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/83834ebc0d95/fnsys-06-00014-a001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/7cb57e507b2d/fnsys-06-00014-a002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/da42df887aa5/fnsys-06-00014-a003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/c002fe0c0b6d/fnsys-06-00014-a004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/8ed4a912277c/fnsys-06-00014-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/81c4e87b7377/fnsys-06-00014-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/0a264b9e48ef/fnsys-06-00014-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/c075fdbf8588/fnsys-06-00014-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/aff3ac50725c/fnsys-06-00014-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/83834ebc0d95/fnsys-06-00014-a001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/7cb57e507b2d/fnsys-06-00014-a002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/da42df887aa5/fnsys-06-00014-a003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce27/3312100/c002fe0c0b6d/fnsys-06-00014-a004.jpg

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