CA200799 CellAura fluorescent H1 antagonist [mepyramine]

(HB7824)

Product overview

  • Name
    CA200799 CellAura fluorescent H1 antagonist [mepyramine]
  • Short description
    Fluorescent H1 histamine receptor antagonist
  • Biological description
    Fluorescent H1 histamine receptor antagonist (apparent KD values are 8.07, 5.37 and >6 for H1, H2 and H3 receptors respectively). Also antagonizes the activity of Histamine, a H1 histamine receptor agonist. Displays no intrinsic activity. A fluorescent mepyramine analogue.
  • Alternative names
    CA200799|H1-BY633-AN|Mempyramine-Bodipy630-650
  • Biological action
    Antagonist
  • Purity
    >97%
  • Citations

Images

Properties

  • Molecular Weight
    948
  • Source
    Synthetic
  • Formulation
    Lyophilized film
  • Excitation
    633 nm
  • Emission
    650 nm

Applications

  • Application notes
    For imaging at the H1 receptor use solutions up to 100 nM.
  • Pharmacological validation

    The CellAura fluorescent H1 antagonist [mepyramine] ligand was shown to antagonize the activity of the H1 agonist, histamine, in the recombinant CHO cell line expressing the human H1 receptor, co-transfected with a serum response element-induced secreted placental alkaline phosphatase (SPAP) reporter gene.

    For the H1 expressing cell line, the serum-induced expression of SPAP was measured under basal and 1% serum-stimulated (maximal) conditions.

    Addition of CellAura fluorescent H1 antagonist [mepyramine] to the basal or serum-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent H1 antagonist [mepyramine] has no intrinsic agonist activity.

    To determine the apparent KD for CellAura fluorescent H1 antagonist [mepyramine] at histamine H1 receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1µM CellAura fluorescent H1 antagonist [mepyramine], and the serum-induced expression of SPAP measured. The apparent KD at H1 was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent H1 antagonist [mepyramine], compared to the response curve for the agonist alone.

    Similar studies were conducted with the CellAura fluorescent H1 antagonist [mepyramine] ligand using recombinant CHO cell lines expressing either the human H2 receptor or the human H3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene. The apparent KD at H2 was calculated in the same way to that calculated for the human H1 receptor.

Storing and Using Your Product

  • 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.