CA200992 CellAura fluorescent 5-HT1A antagonist [NAN-190]

(HB7828)

Product overview

  • Name
    CA200992 CellAura fluorescent 5-HT1A antagonist [NAN-190]
  • Short description
    Fluorescent 5-HT1A receptor antagonist
  • Biological description
    Fluorescent 5-HT1A serotonin receptor antagonist (apparent KD values are 8.75, 6.34 and 5.57 for 5-HT1A, 5-HT2A and 5-HT1B receptors respectively). Antagonizes the activity of serotonin, a 5-HT1A agonist.
  • Alternative names
    CA200992|5HT1A-633-AN2
  • Biological action
    Antagonist
  • Purity
    >97%
  • Citations

Images

Properties

  • Molecular Weight
    1025
  • Source
    Synthetic
  • Formulation
    Lyophilized film
  • Excitation
    633 nm
  • Emission
    650 nm

Applications

  • Application notes
    For imaging at the 5-HT1A receptor use solutions up to 200 nM.
  • Pharmacological validation
    The CellAura fluorescent 5-HT1A antagonist [NAN-190] ligand was shown to antagonize the activity of the 5‑HT1A agonist, 5-HT, in the CHO cell line expressing the human 5-HT1A receptor, using the Ca2+ sensitive fluorescent indicator, Fura-2 AM. Cells were plated in clear bottom black 96-well tissue culture plates and grown to confluence for 24 hours. Medium was then removed and cells incubated in loading buffer comprising HEPES buffered saline with 0.5mM Brilliant Black BN, 2.5mM probenecid, 0.023% pluronic acid F-127 and 2.5µg/ml Fura-2 AM at 37ºC for 30 – 45 mins, either in the presence of CellAura fluorescent 5-HT1A antagonist [NAN-190] or a DMSO vehicle control. During this time serial dilutions of the 5‑HT1A agonist, 5-HT, were prepared in HEPES buffered saline containing 2.5mM probenecid and 0.5mM Brilliant Black BN. To determine the antagonist activity of CellAura fluorescent 5-HT1A antagonist [NAN-190], serial dilutions of the agonist was added to wells with or without CellAura fluorescent 5-HT1A antagonist [NAN-190]. The agonist Ca2+ response in the absence or presence of CellAura fluorescent 5-HT1A antagonist [NAN-190] was determined on a Molecular Devices FlexStation by exciting at 340 nm and 380 nm and ratioing the fluorescence intensity of Fura-2 signal collected at 320 nm. The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent 5-HT1A antagonist [NAN-190], compared to the response curve for the agonist alone.

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.