Discovery of naphthalimide conjugates as fluorescent probes for α1-adrenoceptors

作者：Zhang, Wei; Zhou, Xin-Yang; Yu, Qin-Ying; Du, Lu-Pei; Li, Min-Yong^*

来源：Chinese Chemical Letters, 2016, 27(2): 185-189.

DOI：10.1016/j.cclet.2015.12.002

• alpha(1)-Adrenergic receptors
• Fluorescent probes
• High affinity
• Cell imaging

alpha(1)-Adrenoceptors (alpha(1)-ARs), including at least three subtypes, alpha(1A), alpha(1B) and alpha(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 napthalienide-based small-molecule fluorescent probes (1a -1f) for alpha(1)-ARs, including two parts, a pharmacophore (quinazoline and phenylpiperazine) for alpha(1)-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 alpha(1)-aradrenoceptors.

• 出版日期2016-2
• 单位山东大学