Help Privacy Policy Disclaimer
  Advanced SearchBrowse




Journal Article

Synthesis and properties of fluorescent ß-adrenoceptor ligands


Hallmann,  Dieter
Department of Membrane Biophysics, MPI for biophysical chemistry, Max Planck Society;


Reiländer,  Helmut
Department of Molecular Membrane Biology, Max Planck Institute of Biophysics, Max Planck Society;


Arndt-Jovin,  Donna J.
Department of Molecular Biology, MPI for biophysical chemistry, Max Planck Society;


Jovin,  Thomas M.
Department of Molecular Biology, MPI for biophysical chemistry, Max Planck Society;

External Resource
No external resources are shared
Fulltext (restricted access)
There are currently no full texts shared for your IP range.
Fulltext (public)
There are no public fulltexts stored in PuRe
Supplementary Material (public)
There is no public supplementary material available

Heithier, H., Hallmann, D., Boege, F., Reiländer, H., Dees, C., Jaeggi, K. D., et al. (1994). Synthesis and properties of fluorescent ß-adrenoceptor ligands. Biochemistry, 33(31), 9126-9134. doi:10.1021/bi00197a015.

Cite as: https://hdl.handle.net/21.11116/0000-0007-B39A-1
We describe the synthesis of bordifluoropyrromethene (BODIPY), fluorescein, and related fluorescent derivatives of the beta-adrenergic ligand CGP 12177. With these probes we screened insect (Sf9) cells stably transformed with the human ß2-adrenoceptor gene and expressing (2-3.5) x 105 human ß2-adrenoceptors per cell. Among these derivatives only BODIPY-CGP gave a receptor-specific signal sufficiently strong for measuring the on- and off-rate constants and the equilibrium dissociation constant of beta-adrenoceptor-specific binding by spectrofluorometry or photon counting. Similar KD values for BODIPY-CGP binding were obtained by kinetic measurements (approx. 250 pM) and under equilibrium conditions (400 +/- 180 pM), and these were in the same range as those obtained with [3H]CGP 12177 (200 +/- 32 pM). The cell-bound fluorescence could be quenched specifically with nonfluorescent CGP 12177 to near background levels. The disposition of the ß2-adrenoceptors in BODIPY-CGP-stained Sf9 cells was mainly restricted to the cell surface at 4 and 30 degrees C. Hence, beta-adrenoceptor-expressing cells can be stained specifically with BODIPY-CGP, and beta-adrenoceptors on a single cell can be assessed by photon counting under the fluorescence microscope. Cells can also be scanned by fluorescence-activated flow cytometry.