ChemiScreen™ α1A Adrenoceptor Receptor Stable Cell Line

The endogenous catecholamines, epinephrine and norepinephrine, have profound effects on smooth muscle activity, cardiac function, carbohydrate and fat metabolism, hormone secretion, neurotransmitter release, and central nervous system actions. These activities are mediated by GPCRs belonging to two subfamilies, the α- and β-adrenoceptors (Bylund et al., 1994). The three members of the α1 subclass of adrenoceptors, α1A, α1B and α1D, couple to Gq, and promote contraction of vascular and urinary tract smooth muscle, relaxation of intestinal smooth muscle, increased contractile force in the heart, and glycogenolysis and gluconeogenesis in the liver. The different subtypes have overlapping distributions and variably contribute to these effects depending on species and tissue; the α1A subtype plays a prominent role in urogenital smooth muscle contraction and renal artery contraction (Hrometz et al., 1999; Ruffolo and Hieble, 1999). Activation of a1 adrenoceptors also influences cell proliferation; α1A inhibits cell growth by arresting progression at the G1/S transition (Shibata et al., 2003). The α1A subtype undergoes alternative splicing to generate four variants that differ at their C-termini, although these variants appear to be functionally identical (Chang et al., 1998). Cloned human α1A receptor-expressing ChemiScreen cells were constructed by stable transfection of Chem-1 cells with α1A. These stability-tested cells are ready for fluorescence-based assays for agonists, antagonists and modulators at the α1A receptor.

Catalog No. Size Price Quantity
HTS087C 2 Vials $18,779.00

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Application
Calcium Flux Assay
Family
Adrenoceptor
Target
α1A
Accession Number
NM_000680
Species
Human
Host Cell Type
Chem-1
Content
2 Vials of mycoplasma-free cells, 1 ml per vial
Storage
Cell vials are to be stored in the vapor phase of liquid N2.
  • [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines

    The ChemiSCREEN and ChemiBRITE Cell Lines are designed to enable the measurement of intracellular calcium levels when a GPCR of interest has been activated by a ligand. These cell lines are suitable for studying small molecules as well as biologics. The assay protocol has been optimized for use in either a 384-well or 96-well format.

    ChemiSCREEN and ChemiBRITE cells stably expres...

    [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines