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Histamine H1 receptor ligand binding assay

Histamine H1 binding assay starter pack

Products Product reference Product insert MSDS
Histamine H1 receptor green inv ago-5,000 tests L0015GRE pdf pdf
Tag-lite Histamine H1 - 1 Million labeled cells C1TT1H1 pdf -
Tag-lite buffer - 100 ml (5X) LABMED - -

The binding assay starter pack consists of three references, the labeled cells, the fluorescent ligand and the Tag-lite buffer. Each component must be ordered separately. The cells express the SNAP-receptor labeled with terbium cryptate (labeling performed with Tag-lite SNAP-Lumi4 Tb). The labeled cells are proposed in a 1 million cell pack, to achieve a minimum of 100 tests at a cell density of 10,000 cells/well.

Features:
  • This inverse agonist is a Mepyramine derivative labeled with a Green Emitting HTRF fluorescent probe
  • This ligand has been successfully used in a Histamine H1 receptor Tag-lite binding assay
  • Developed under collaboration with CellAura
  • Concentration: 20µM
  • Volume: 250µL
  • Buffer: HEPES 50mM, pH7.4 + 10%DMSO
  • Molecular Weight: 874
Related products Product reference Product insert
Plasmid pSNAP-H1 PSNAPH1 pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -

Assay Validation:

 

Histamine H1 receptor ligand binding assay was performed using the starter pack reagents.

Kd was determined, and signal inhibition (IC50) by agonist and antagonist was performed with L0015GRE (Tag-lite Histamine H1 receptor green inverse agonist) 50nM.

Results obtained with radioligand assay and Tag-lite platform were very similar.

Family Receptor Compounds (antagonist) Radioactivity
(Ki nM)
Tag-lite
(Ki nM)
Histamine H1 Triprolidine 1.53 (1) 1.51
Doxepin 0.32 (1) 0.65

Booth et al, J Pharmacol Exp Ther, 2002



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