5-Hydroxytryptamine (Serotonin) Receptor 4 (HTR4) ACTOne Stable Cell Line
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Catalog Number:
CL-01-HTR4
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In Stock
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Price: Please inquire order@eEnzyme.com
Detailed Description
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CL-01-HTR4
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Name
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5-Hydroxytryptamine (Serotonin) Receptor 4 (HTR4) ACTOneTM Stable Cell Line
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Description
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This cell line is a HEK-293-CNG cell line that expresses a recombinant human HTR4. HEK-293-CNG cells express a modified CNG (Cyclic Nucleotide Gated) channel that opens in response to elevated intracellular cAMP levels and consequently result in ion flux and cell membrane depolarization. The assay allows both end-point and kinetic measurement of intracellular cAMP changes with a FLIPR or a fluorescence microplate reader.
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Application
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cAMP dependent human HTR4 cell-based assay;
Cell-based high-throughput screening (HTS) of human HTR4 agonists/antagonists
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Size
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1 mL (frozen cells; 1x 106 cells before freezing)
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Detection
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FlexStation or Microplate reader
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Detection
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==>> DATA SHEET ==>> MSDS
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Synonym: 5-Hydroxytryptamine Receptor 4, 5-HT4, 5-Hydroxytryptamine (Serotonin) Receptor 4 G Protein-Coupled, 5-Hydroxytryptamine (Serotonin) Receptor 4, Cardiac 5-HT4 Receptor, Serotonin Receptor 4, 5-HT4R, 5-HT-4
About Human 5-Hydroxytryptamine Receptor 4 (HTR4/5-HT4R) Stable Cell Line
5-Hydroxytryptamine Receptor 4 (HTR4), commonly known as the 5-HT4 receptor (5-HT4R), is a Class A G protein-coupled receptor (GPCR) that is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). HTR4 primarily couples to Gs proteins, stimulating adenylate cyclase activity and increasing intracellular cAMP levels. The receptor is expressed throughout the central nervous system and in peripheral tissues, including the gastrointestinal tract, heart, and urinary bladder, where it regulates neurotransmission, gastrointestinal motility, cardiac function, and smooth muscle activity.
HTR4 plays important roles in learning, memory, cognition, gastrointestinal transit, and neurotransmitter release. Dysregulation of HTR4 signaling has been implicated in irritable bowel syndrome (IBS), chronic constipation, Alzheimer's disease, depression, and other neurological disorders. Consequently, HTR4 has become an important therapeutic target for both gastrointestinal and central nervous system drug discovery.
eEnzyme's Human HTR4 Stable Cell Line provides a reliable platform for investigating HTR4-mediated signaling and evaluating agonists, antagonists, partial agonists, and novel receptor modulators using cAMP and other GPCR functional assays. The cell line is well suited for receptor characterization, compound profiling, potency determination, and high-throughput drug screening.
Applications
• HTR4 (5-HT4R) receptor pharmacology studies
• Serotonin signaling research
• Agonist and antagonist screening
• Gastrointestinal motility research
• IBS and chronic constipation drug discovery
• Neurodegenerative and cognitive disorder studies
• cAMP and GPCR functional assays
• High-throughput screening (HTS)
Biological Significance of HTR4
HTR4 is an important mediator of serotonin signaling in both the central and peripheral nervous systems. Activation of the receptor stimulates cAMP production through Gs-mediated signaling, enhancing neurotransmitter release, synaptic plasticity, gastrointestinal motility, and cognitive function. Clinically, selective HTR4 agonists have been developed to treat gastrointestinal motility disorders, while emerging evidence suggests that modulation of HTR4 may provide therapeutic benefits for Alzheimer's disease, depression, and cognitive impairment. Because of its diverse physiological functions and therapeutic potential, HTR4 remains an attractive target for neuroscience, gastroenterology, and GPCR-focused drug discovery. The HTR4 Stable Cell Line provides a valuable tool for studying serotonin receptor biology and accelerating the development of next-generation therapeutics.
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