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Reagent Details

Dopamine family

Catalogue number: CA200766
Product: D1 antagonist [SKF-83566-like]
Selectivity: D1:6.71 (to be phased out)

Pharmacophore  SKF83566-like-derivative
Molecular Weight   956
Purity   ≥97%
Excitation   633 nm
Emission   650 nm

 

Imaging information

For imaging at the D1 receptor use solutions up to 100 nM.

Pharmacological Validation

The CA200766 ligand was shown to antagonize the activity of the D1 agonist, SKF 83566, in a recombinant CHO cell line expressing the human D1 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.

The cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions (below-left). Addition of CA200766 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CA200766 has no intrinsic agonist activity.

To determine the apparent KD for CA200766, cells were treated with varying concentrations of SKF 83566 alone, or in the presence of 1µM CA200766, 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 CA200766, compared to the response curve for the agonist alone.

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