HUMAN RECOMBINANT 5-HT2A RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Full-length Human HTR2A cDNA (GenBank Accession Number NM_000621) with FLAG-tag sequence at the N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DME/F12, 10% FBS, 10 ug/mL puromycin
Stable after minimum two months continuous growth
Background: 5-HT2A (5-hydroxytryptamine receptor 2A) is a receptor for serotonin. It is expressed throughout the central nervous system in the neocortex and olfactory tubercle. Additionally, it is expressed in platelets, fibroblasts and neurons of the peripheral nervous system. 5-HT2A receptor agonists may have important clinical value in the treatment of various disorders, such as depression, anxiety, bipolar disorder and schizophrenia. It is also a receptor for the human polyomavirus, JC virus.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MULTISCREENTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose- dependent stimulation of intracellular IP1 accumulation upon treatment with ligand, measured with IP-one Tb kit. Figure 3. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP accumulation upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01) Figure 4. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Meltzer and Li (2003) Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 27:1159-1172.
Porter et al. (1999) Functional characterization of agonists at recombinant human 5- HT2A, 5-HT2B, and 5-HT2C receptors in CHO-K1 cells. Br J Pharmacol 128:13-20.
Stam et al. (1992) Genomic organization, coding sequence and functional expression of human 5-HT2 and HT1A receptor genes. Eur J Pharmacol 227:158-162.