摘要
α1-Adrenoceptors（α1-ARs）, including at least three subtypes, α（1A）, α（1B） and α（1D）, which play essential roles in G protein-coupled receptors（GPCRs）, can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes（1a-1f） for α1-ARs, including two parts, a pharmacophore（quinazoline and phenylpiperazine） for α1-AR recognition and a fluorophore（naphthalimide） for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α1-adrenoceptors.
α1-Adrenoceptors（α1-ARs）, including at least three subtypes, α（1A）, α（1B） and α（1D）, which play essential roles in G protein-coupled receptors（GPCRs）, can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes（1a-1f） for α1-ARs, including two parts, a pharmacophore（quinazoline and phenylpiperazine） for α1-AR recognition and a fluorophore（naphthalimide） for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α1-adrenoceptors.
基金
supported by grants from the Fok Ying Tong Education Foundation (No. 122036)
the Program of New Century Excellent Talents in University (No. NCET-11-0306)
the Shandong Natural Science Foundation (No. JQ201019)
the Independent Innovation Foundation of Shandong University, IIFSDU (No. 2010JQ005)
