Corticotropin-Releasing Hormone Receptor 1 (CRHR1) ACTOneTM Stable Cell

Catalog Number:
CL-01-CRHR1
In Stock
Price: Please inquire order@eEnzyme.com
Detailed Description

CL-01-CRHR1

Name

Corticotropin-Releasing Hormone Receptor 1 (CRHR1) ACTOneTM Stable Cell Line

Description

This cell line is a HEK-293-CNG cell line that expresses a recombinant human CRHR1. 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.

Application

cAMP dependent human CRHR1 cell-based assay;

cell-based high-throughput screening of human CRHR1 agonists/antagonists.

Size

1x 106 cells

Detection

FlexStation or Microplate reader

For Downloading

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About Human Corticotropin-Releasing Hormone Receptor 1 (CRHR1/CRF1) Stable Cell Line

Corticotropin-Releasing Hormone Receptor 1 (CRHR1), also known as CRF1 receptor, is a Class B G protein-coupled receptor (GPCR) that serves as the primary receptor for corticotropin-releasing hormone (CRH, also known as CRF) and related peptides of the urocortin family. CRHR1 is widely expressed throughout the central nervous system, particularly in the hypothalamus, cerebral cortex, amygdala, hippocampus, pituitary gland, and other regions involved in stress regulation, emotional processing, and neuroendocrine control. Upon activation by CRH, CRHR1 primarily couples to Gs proteins, stimulating adenylate cyclase activity and increasing intracellular cAMP levels, thereby regulating downstream signaling pathways that coordinate physiological and behavioral responses to stress.

CRHR1 is a key component of the hypothalamic-pituitary-adrenal (HPA) axis, the body's principal neuroendocrine stress response system. Activation of CRHR1 in the anterior pituitary stimulates adrenocorticotropic hormone (ACTH) release, leading to glucocorticoid production by the adrenal glands. Beyond endocrine regulation, CRHR1 signaling influences anxiety, depression, cognition, emotional behavior, pain perception, immune responses, and gastrointestinal function. Dysregulation of CRHR1 signaling has been implicated in major depressive disorder, anxiety disorders, post-traumatic stress disorder (PTSD), addiction, irritable bowel syndrome (IBS), and other stress-related diseases, making CRHR1 an important therapeutic target in neuroscience and psychiatry.

eEnzyme's Human CRHR1 Stable Cell Line provides a reliable and reproducible cellular platform for investigating CRHR1-mediated signaling pathways and evaluating receptor-targeted therapeutics. The cell line enables quantitative assessment of CRH peptides, urocortins, agonists, antagonists, and novel receptor modulators through cAMP assays, reporter gene assays, and other GPCR functional screening platforms. Researchers can utilize this stable cell line for receptor characterization, ligand profiling, potency determination, lead optimization, and high-throughput screening applications supporting neuroscience, endocrinology, and psychiatric drug discovery programs.

Applications of the CRHR1 Stable Cell Line

• CRHR1 receptor pharmacology studies
• CRH and urocortin signaling investigations
• Agonist and antagonist screening
• Stress biology and HPA axis research
• Anxiety and depression studies
• PTSD and neuropsychiatric disorder research
• cAMP and GPCR functional assays
• High-throughput screening applications

Biological Significance of CRHR1

CRHR1 is a master regulator of the physiological response to stress and plays a central role in coordinating neuroendocrine, behavioral, and autonomic adaptations to environmental challenges. Activation of CRHR1 stimulates ACTH secretion and glucocorticoid production, helping the body respond to acute stressors. Within the brain, CRHR1 signaling influences emotional behavior, fear processing, cognition, arousal, and mood regulation. Chronic overactivation of the CRH-CRHR1 pathway has been linked to anxiety disorders, depression, PTSD, substance abuse disorders, and stress-related gastrointestinal dysfunction. Consequently, CRHR1 has been extensively investigated as a therapeutic target for psychiatric and stress-associated diseases. Because of its pivotal role in stress physiology and neuroendocrine regulation, CRHR1 remains an important focus of translational research and CNS drug discovery. The CRHR1 Stable Cell Line provides a valuable tool for studying receptor biology and advancing the development of next-generation therapeutics targeting stress-related and neuropsychiatric disorders.

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