Selective fluorescent D1 dopamine receptor antagonist (apparent KD values are 7.09, < 5 and 7.56 for D1, D2 and D5 receptors respectively). Also antagonizes the activity of SKF 83566, a D1 dopamine receptor agonist. Displays no intrinsic agonist activity.
For imaging at the D1 receptor use solutions up to 100 nM.
Pharmacological validation
The CellAura fluorescent D1 antagonist [SKF83566-green] 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 CellAura fluorescent D1 antagonist [SKF83566-green] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent D1 antagonist [SKF83566-green] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent D1 antagonist [SKF83566-green], cells were treated with varying concentrations of SKF 83566 alone, or in the presence of 1µM CellAura fluorescent D1 antagonist [SKF83566-green], 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 CellAura fluorescent D1 antagonist [SKF83566-green], compared to the response curve for the agonist alone.
Solubility & Handling
Storage instructions
-20°C (protect from light)
Solubility overview
Soluble in DMSO
Handling
After thawing individual aliquots for use, we recommend briefly sonicating the sample to ensure it is fully dissolved and the solution is homogeneous. We do not recommend using the product after subjecting it to repetitive freeze-thaw cycles.
Shipping conditions
The product, supplied in a dry form, is stable at ambient temperature for periods of up to a few days and does not require shipping on ice/dry ice.
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.