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Reagent Details

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Catalogue number: CA200773
Product: D1 antagonist [SKF83566-green]
Selectivity: D1: 7.09 | D2: < 5.0 | D5: 7.56

Labelled with BODIPY-FL (green)

 

Pharmacophore SKF83566-derivative Catalogue Number Pack Size Price
Molecular Weight 877 CA200773-TK0* 0.05 mg £137.50*
Purity ≥97% CA200773-020 0.2 mg £500
Excitation 488 nm CA200773-050 0.5 mg £1200
Emission 525 nm CA200773-100 1.0 mg £2150

 

 
* Ordered as part of a TestKit comprising a selection of 4 ligands, listing 4 catalogue numbers ending in -TK0
 

 

Imaging information

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

Pharmacological Validation

The CA200773 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. Addition of CA200773 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CA200773 has no intrinsic agonist activity.

To determine the apparent KD for CA200773, cells were treated with varying concentrations of SKF 83566 alone, or in the presence of 1µM CA200773, 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 CA200773, compared to the response curve for the agonist alone.

 

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