Corticotropin-Releasing Hormone GPCR Assays
Overview of Corticotropin-releasing Hormone (CRH) Receptors
CRH, an important regulator of immunity, neurosecretion, and endocrine, can stimulate the secretion of adrenocorticotropic hormone and glucocorticoid. The biological effects of CRH are mediated by binding to two G protein-coupled receptors (GPCRs), CRHR1 and CRHR2, each with unique splicing patterns and markedly different pharmacological properties.
Fig.1. Schematic representation of the CRHR2 targeted pathways. (Rodriguez, 2015)
Distribution of CRH Receptors
CRH receptors are widely expressed in the central nervous system and periphery in humans as well as rodents and other mammals, and they play a key role in integrating stress responses and coordinating activities. Studies have found that CRHR1 is highly expressed in the cerebral cortex, cerebellum, and hippocampus, and is also widely expressed in human peripheral tissues, such as the ovary, myometrium, placenta, testis, adrenal gland, skin, heart, and specific cells of the immune system. CRHR2 is expressed in discrete patterns in the brain. In addition, CRHR2 is also abundant in peripheral tissues of the skin and skeletal muscle, smooth muscle, and cardiac muscle.
Implications of CRH Receptors
The ability of CRH receptors to couple to multiple G proteins and regulate multiple intracellular networks enables them to play unique roles in the regulation of homeostatic mechanisms.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| CRH type 1 receptor | CRHR1 |
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| CRH type 2 receptor | CRHR2 |
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Assay List of Corticotropin-Releasing Hormone Receptors
Creative Biolabs can provide a range of assays of corticotropin-releasing hormone receptors. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title | Dysregulation of bladder corticotropin-releasing hormone receptor in the pathogenesis of human interstitial cystitis/bladder pain syndrome |
| Journal | Scientific reports |
| Published | 2019 |
| Abstract | Stress is strongly associated with worsening symptoms in patients with interstitial cystitis/bladder pain syndrome (IC/BPS). To investigate the mechanism by which stress is associated with IC/BPS, researchers investigated the expression of the stress response receptor CRHR in the bladder of IC/BPS patients. Obtain cystoscopic biopsy of bladder wall including mucosa and submucosa from target patients. Bladder expression of CRHR1 and CRHR2 was characterized by western blot. Immunochemical staining results showed that CRHR1 expression was mainly located in the submucosa, while CRHR2 expression was mainly located in urothelial cells. Compared with controls, IC/BPS patients showed significantly increased CRHR1 expression, while CRHR2 expression was significantly decreased. |
| Result |
The findings of this article demonstrated differential CRHR expression in the bladder urothelium and suburothelium of IC/BPS patients. The expression of CRHR1 in IC/BPS patients was significantly positively correlated with nerve growth factor (NGF) and negatively correlated with E-cadherin. Although more effort is needed to address the impact of CRHR signaling, alterations in receptor expression suggest a potential role for CRH-related peptides within the bladder mucosa in IC/BPS pathophysiology.
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Fig.2. The double immunochemical staining of CRHR1 and tryptase in the bladder of IC/BPS patients. (Jhang, 2019)
References
- Rodriguez, J. A.; et al. Diminished expression of corticotropin-releasing hormone receptor 2 in human colon cancer promotes tumor growth and epithelial-to-mesenchymal transition via persistent interleukin-6/STAT3 signaling. Cellular and Molecular Gastroenterology and Hepatology. 2015; 1(6): 610-630.
- Jhang, J.F.; et al. Dysregulation of bladder corticotropin-releasing hormone receptor in the pathogenesis of human interstitial cystitis/bladder pain syndrome. Scientific reports. 2019; 9(1): 1-8.
