Corticotropin-releasing hormone receptors (CRHRs) are a type of G-protein coupled receptor found in mammals that bind with corticotropin-releasing hormone (CRH) and mediate its biological effects. CRH is a key hormone involved in the stress response and plays a crucial role in regulating various physiological processes, such as the activation of the hypothalamic-pituitary-adrenal axis and the release of glucocorticoid hormones.
CRHRs are primarily divided into two subtypes, CRHR1 and CRHR2. CRHR1 is predominantly located in the cortical region of the brain, including the hippocampus, amygdala, and cerebral cortex. Activation of CRHR1 receptors leads to the release of adrenocorticotropic hormone (ACTH) from the pituitary gland, triggering the stress response. Moreover, CRHR1's activation is implicated in anxiety and depression disorders.
On the other hand, CRHR2 receptors are found in various brain regions, including the hypothalamus and hippocampus, as well as in peripheral tissues like the heart, kidney, and gastrointestinal tract. The activation of CRHR2 receptors is involved in the modulation of behaviors related to stress, anxiety, appetite, and nociception. There are distinct isoforms of CRHR2, denoted as CRHR2α and CRHR2β, which differ in their tissue distribution and affinity for CRH.
Understanding the function and regulation of CRHRs is crucial for unraveling the intricacies of stress-related disorders and developing pharmacological interventions to modulate their effects. Targeting CRHRs with specific agonists or antagonists has therapeutic potential for various conditions, including anxiety, depression, and metabolic disorders.
