Dautzenberg F M, Kilpatrick G J, Hauger R L, Moreau J
F. Hoffmann-La Roche Ltd., Pharma Division, Preclinical Research Grenzacher Strasse 124, 4070, Basel, Switzerland.
Peptides. 2001 May;22(5):753-60. doi: 10.1016/s0196-9781(01)00388-6.
Dysfunctioning of corticotropin-releasing hormone (CRH) and its receptors (CRH(1) and CRH(2)) has been linked to the development of stress-related disorders, such as mood and eating disorders. The molecular characterization of CRH(1) and CRH(2) receptors and their splice variants has generated detailed information on their pharmacology, tissue distribution and physiology. While mammalian CRH(1) receptors nonselectively bind CRH analogs, the ligand specificity of CRH(2) is narrower. CRH(1) receptors are predominantly expressed in the brain and pituitary, whereas CRH(2) receptor expression is limited to particular brain areas and to some peripheral organs. Molecular approaches to block CRH(1) receptor expression in the brain argue in favor of its involvement in the regulation of some aspects of the stress response. The CRH(2alpha) receptor may be more important for motivational types of behavior essential for survival, such as feeding and defense.(1)
促肾上腺皮质激素释放激素(CRH)及其受体(CRH(1)和CRH(2))功能失调与应激相关疾病的发生有关,如情绪和饮食失调。CRH(1)和CRH(2)受体及其剪接变体的分子特征已产生了有关其药理学、组织分布和生理学的详细信息。虽然哺乳动物的CRH(1)受体非选择性地结合CRH类似物,但CRH(2)的配体特异性更窄。CRH(1)受体主要在脑和垂体中表达,而CRH(2)受体的表达仅限于特定脑区和一些外周器官。在脑中阻断CRH(1)受体表达的分子方法支持其参与应激反应某些方面的调节。CRH(2α)受体对于生存所必需的动机性行为类型,如进食和防御,可能更为重要。(1)