Fluorescent H2 histamine receptor antagonist (apparent KD values are 8.94, 7.3 and >6 for H2, H3 and H1 receptors respectively). Also antagonizes the activity of Histamine, a H1 agonist. Displays no intrinsic activity.
For imaging at the H2 or H3 receptor use solutions up to 100 nM.
Pharmacological validation
The CellAura fluorescent H2 antagonist [aminopotentidine] ligand was shown to antagonize the activity of the agonist, histamine, in a recombinant CHO cell line expressing the human H2 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene, and in a similar cell line expressing the human H3 receptor. No antagonist activity of the CellAura fluorescent H2 antagonist [aminopotentidine] ligand was detected at the highest concentration tested in a recombinant cell line expressing human H1 receptor provided by Applied Cell Sciences (Rockville, MD 20850, USA. Catalogue number: A665). For the H2 and H3 expressing cell lines, the cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. Addition of CellAura fluorescent H2 antagonist [aminopotentidine] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent H2 antagonist [aminopotentidine] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent H2 antagonist [aminopotentidine] at histamine H2 and H3 receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1µM CellAura fluorescent H2 antagonist [aminopotentidine], and the cyclic AMP-induced expression of SPAP measured. The apparent KD at H2 and H3 was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent H2 antagonist [aminopotentidine], 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.
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