HTS132RTA - Ready-to-Assay™ 5-HT2C Serotonin Family Receptor Frozen Cells

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    5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2C, which couples to Gq in most cells to stimulate intracellular calcium, is prominently expressed in brain and appears to modulate depression, anxiety and appetite (Miller, 2005; Serretti et al., 2004; Wood, 2003). The mRNA encoding 5-HT2C undergoes selective RNA editing that changes 4 amino acids in the second intracellular loop; these changes result in alteration of efficiency of coupling to G proteins. Alterations in editing of 5-HT2C have been detected in victims of suicidal depression and in mice treated with the SSRI, fluoxetine (Tohda et al., 2006). Cloned human 5-HT2C -expressing cell line is made in the Chem-1 host, which supports high levels of recombinant 5-HT2C expression on the cell surface for functional detection via the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at 5-HT2C.

    Additional Resource :  HTS132RTA092514 Datasheet

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    Item Unit of Measure: PK
    Quantity: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2. Media Component at 4ºC (-20ºC for prolonged storage).
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exongenous Gene Expression: HTR2C cDNA (Accession Number: NM_000868- see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Barnes NM and Sharp T (1999) A review of central 5-HT receptors and their function. Neuropharmacology, 38, 1083-1152.
    Reference 2: 2. Miller KJ (2005) Serotonin 5-HT2C receptor agonists: potential for the treatment of obesity. Mol. Interv. 5: 282-91.
    Reference 3: 3. Serretti A et al. (2004) The 5-HT2C receptor as a target for mood disorders. Expert Opin. Ther. Targets 8: 15-23.
    Reference 4: 4. Tohda M et al. (2006) The molecular pathopharmacology of 5-HT2C receptors and the RNA editing in the brain. J. Pharmacol. Sci. 100: 427-432.
    Reference 5: 5. Wood (2003) Therapeutic potential of 5-HT2C receptor antagonists in the treatment of anxiety disorders. Curr. Drug Targets CNS Neurol. Disord. 2: 383-7.