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Histamine receptor H1 (H1) - HRH1

Target Class GPCR FamilyHistamine
SpeciesHuman   
Background
Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3 and H4. This gene was thought to be intronless until recently. The protein encoded by this gene is an integral membrane protein and belongs to the G protein-coupled receptor superfamily. It mediates the contraction of smooth muscles, the increase in capillary permeability due to contraction of terminal venules, the release of catecholamine from adrenal medulla, and neurotransmission in the central nervous system. Multiple alternatively spliced variants, encoding the same protein, have been identified. [provided by RefSeq, Jul 2008]

Cell Background
CHO-K1
Readout
Calcium
Method
Detect calcium mobilization using DiscoverX Calcium No WashPLUS
Agonist/Ligand
Histamine
Agonist/Ligand EC50
42
Agonist Effect (Activation)
decrease BP; allergic responses of flare, flush, and wheal; bronchoconstriction
Antagonist Effect (Inhibition)
sedation; decrease allergic responses; increase body weight
Ref.
Bowes et. al. 2012
AgonistEC50(nM)
Histamine42
Methylhistaprodifen 135
AntagonistIC50(nM)
Diphenhydramine44
Doxepin0.7
Promethazine1.3
Pyrilamine 3.8
Cells are plated in a 384-well plate and incubated overnight at 37°C/5% CO2 to allow the cells to attach and grow. Cells are then stimulated with a control agonist. Following stimulation, calcium mobilization is detected using the Calcium No WashPLUS detection kit.
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