HUMAN RECOMBINANT H2 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human HRH2 cDNA (GenBank accession number NM_022304.2) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Background: Histamine is one of the most studied biomolecules in medicine and is most notably known for its effects on smooth muscle contraction, vascular permeability and regulation of stomach acid. H2 receptors are positively coupled to adenylate cyclase via Gs. It increases the intracellular Ca2+ concentrations and release Ca2+ from intracellular stores by coupling to Gq. H2 receptors have been found to be located in a variety of tissues, including the brain, gastric cells, and cardiac tissue. Histamine H2 receptors have a potent effect on gastric acid secretion, and the inhibition of this secretory process by H2 receptor antagonists has provided evidence for an important physiological role of histamine in the regulation of gastric secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation. It has also been demonstrated to control the relaxation of smooth muscles.
Application: Functional assays
Figure 1. a) Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). b) Dose-dependent inhibition of calcium flux upon treatment with antagonist, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent stimulation of intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Hill, S.J. et al. (1997) Classification of Histamine Receptors. Pharmacological Reviews vol 49 no. 3 253-278
Martínez-Mir, M. I et al. (1992) Effect of histamine and histamine analogues on human isolated myometrial strips. Br J Pharmacol, 107: 528-531.