Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 5, Pages 502-506Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml5004298
Keywords
alpha(1)-Adrenergic receptors; fluorescent probes; quinazoline; cell imaging; subcellular localization
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Funding
- Fok Ying Tong Education Foundation [122036]
- Program of New Century Excellent Talents in University [NCET-11-0306]
- Shandong Natural Science Foundation [JQ201019]
- Independent Innovation Foundation of Shandong University, IIFSDU [2010JQ005]
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alpha(1)-Adrenergic receptors (alpha(1)-ARs), as the essential members of G protein-coupled receptors (GPCRs), can mediate numerous physiological responses in the sympathetic nervous system. In the current research, a series of quinazoline-based small-molecule fluorescent probes to alpha(1)-ARs (1a-1e), including two parts, a pharmacophore for alpha(1)-AR recognition and a fluorophore for visualization, were well designed and synthesized. The biological evaluation results displayed that these probes held reasonable fluorescent properties, high affinity, accepted cell toxicity, and excellent subcellular localization imaging potential for alpha(1)-ARs.
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