Human H1 Histamine Receptor Cell Line

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  • Intracellular calcium response from CHO-K1 cells stably expressing human H1 histamine receptors (red) or from untransfected control cells (black). Cells were loaded with Fluo-4NW then stimulated with the indicated concentrations of histamine. Calcium responses were recorded on a FlexStation plate reader. Data represent the average +/- standard deviation of triplicate determinations.
  • Reference Compounds (agonist): Histamine EC50:  4 nM , HTMT EC50: 5,060 nM , 2-pyridylethylamine EC50:  238 nM
  • Reference Compounds (antagonist): Diphenylhydramine IC50:  461 nM , Cetirizine IC50:  417 nM , Astemizole IC50:  111 nM

Human H1 Histamine Receptor Cell Line

  • Cat.#:
  • A665
  • Lot #:
  • 726

Availability: In stock

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Quick Overview

Human H1 Histamine Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.

Background

Histamine is a ubiquitous messenger that mediates a large number of physiological processes. Its actions are mediated by four receptors named H1, H2, H3 and H4 receptors. The H1 histamine receptor is expressed primarily in lung, vasculature and brain where it mediates smooth muscle contraction, food intake and sleep, amongst other actions. Perhaps most notably, antagonists to this receptor are frequently prescribed to treat respiratory allergies.
General Info
Synonyms HRH1
Product Description Human H1 Histamine Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.
Target Type GPCR
Product Type Replicating Cell Line
Receptor Histamine
Sub-Type H1
Therapeutic Area metabolic & gastrointestinal, pain & inflammation
Related Services Membrane Preparation, Large-scale Cryopreservation, GPCR Screening
Genbank Accession Number NM_000861; no expressed tags
Validated Assay/Platform calcium
References Fukui, H et al., (1994) Molecular cloning of the human histamine H1 receptor gene. Biochem. Biophs. Res. Commun. 201: 894-901.
Gelfand, E.W. (2002) Role of histamine in the pathophysiology of asthma: immunomodulatory and anti-inflammatory acti
Host cell CHO-K1
Mycoplasma Status Negative (MycoAlert Kit)
Growth media Ham's F12, 10% FBS, 0.4 mg/mL G418
Storage & Packaging
Packaging Cryopreserved cells, 6 million cells per vial
Storage Recommendation liquid nitrogen
Stability 12 passages (6 weeks of continuous culture)
Quantity 6 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human H1 histamine receptor
Screening Assay calcium mobilization assay
Readout calcium sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 7.04
Z Score 0.72
DMSO Tolerance 1.5% DMSO
Testing Modes agonist, antagonist, PAM
Testing Options 16-point minimum, 4-point DRC (n = 4), 8-point DRC (n=3 or 4)
Turnaround Time 2 weeks following receipt of Test Articles
Product Documentation
Specification Sheet  Download PDF Document
Screening Info  Download PDF Document