Discovery of the First Environment-Sensitive Near-Infrared (NIR) Fluorogenic Ligand for 1-Adrenergic Receptors Imaging in Vivo. Academic Article uri icon


  • Fluorescent ligands are gaining popularity as tools to aid GPCR research. Nonetheless, in vivo application of such tools is hampered due to their short excitation wavelengths in the visible range and lack of fluorogenic switch. Here we report the discovery of fluorescent ligands (3a-f) for 1-adrenergic receptors (1-ARs) by conjugating the environment-sensitive fluorophore cyane 5 (Cy5) with the quinazoline pharmacophore. Among them, the conjugated compound 3a, with acylated piperazine and the shortest carbon chain spacer, exhibited potent binding and remarkable changes in fluorescence (10-fold) upon binding to 1-AR. Furthermore, it could be employed to selectively and specifically label 1-ARs with no washing procedures in single cells, prostate tissue slices, intact tumor xenografts and organs in living mice. Especially, the slice imaging results gave direct and visual evidence that there is a close relationship between 1-ARs and pathological prostate. It is anticipated that our fluorescent tools will find broad applications in the study of 1-AR pharmacology and physiology to aid development of novel therapeutics.

published proceedings

  • J Med Chem

author list (cited authors)

  • Ma, Z., Lin, Y., Cheng, Y., Wu, W., Cai, R., Chen, S., ... Li, M.

citation count

  • 25

complete list of authors

  • Ma, Zhao||Lin, Yuxing||Cheng, Yanna||Wu, Wenxiao||Cai, Rong||Chen, Shouzhen||Shi, Benkang||Han, Bo||Shi, Xiaodong||Zhou, Yubin||Du, Lupei||Li, Minyong

publication date

  • March 2016