Reagent Details

Applications

For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.

Pharmacological Validation

The CA200656 ligand was shown to antagonize the activity of the non-selective β agonist, isoprenaline, in three separate recombinant CHO cell lines expressing either the human β1, β2 or β3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.

The CA200656 ligand was shown to antagonize the activity of the non-selective β agonist, isoprenaline, in three separate recombinant CHO cell lines expressing either the human β1, β2 or β3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.

To determine the apparent KD for CA200656 at β1, β2 and β3 receptors, cells were treated with varying concentrations of isoprenaline alone, or in the presence of 1µM CA200656, and the cyclic AMP-induced expression of SPAP measured.

The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of CA200656, compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines.

Cell Lines: 
A+B, HEK cells expressing endogenous β2 adrenoceptors provided by Perkin-Elmer Cellular Technologies, Hamburg, Germany.
C+D, CHO-K1 cells expressing recombinant β2 adrenoceptors provided by ChanTest, Rockville, MD 20850, USA. (Catalogue number: A600)
E+F, CHO cells expressing recombinant β2 adrenoceptors provided by Institute of Cell Signaling, University of Nottingham, UK.