Corticotropin-releasing hormone receptors (CRHRs), also known as corticotropin-releasing factor receptors (CRFRs) are a G protein-coupled receptor family that binds corticotropin-releasing hormone (CRH). There are two receptors in the family, designated as type I and 2, each encoded by a separate gene (CRHR1 and CRHR2 respectively).
CRHRs are important mediators in the stress response. Cells in the anterior lobe of the pituitary gland known as corticotropes express the receptors and will secrete adrenocorticotropic hormone (ACTH) when stimulated. This binding of Corticotropin Releasing-Hormone (CRH) activates the hypothalamic pituitary adrenal axis (HPA axis), one of the 2 parts of the fight or flight response to stress. CRHRs are also present in other brain areas such as the amygdala, locus coeruleus and hippocampus. Within the hippocampus, the CRHR1s are most abundant, residing mainly on the pyramidal cells of CA1 and CA3. Chronic activation of CRHR1s by CRH induced by early life stress has been shown to underlie memory deficits and learning impairments and anxiety in adulthood.
- ^ Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM (2003). "International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands". Pharmacol. Rev. 55 (1): 21–6. PMID 12615952. doi:10.1124/pr.55.1.3.
- ^ Grammatopoulos DK, Chrousos GP (2002). "Functional characteristics of CRH receptors and potential clinical applications of CRH-receptor antagonists". Trends Endocrinol. Metab. 13 (10): 436–44. PMID 12431840. doi:10.1016/S1043-2760(02)00670-7.
- ^ Aguilera G, Wynn PC, Harwood JP, Hauger RL, Millan MA, Grewe C, Catt KJ (1986). "Receptor-mediated actions of corticotropin-releasing factor in pituitary gland and nervous system". Neuroendocrinology 43 (1): 79–88. PMID 3012395. doi:10.1159/000124513.
- Antagonists: Aprepitant
- Nolpitantium besilate
- SDZ NKT 343
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